Medicinal chemistry and pharmaceutical chemistry

Md. Reyad-ul-Ferdous, Mosharaf Hossen, Nasir Uddin, Md. Saiful Islam Arman, Ariful Islam, Sujan Bose Nature is the abundant source of medicines. All plants contents lots of chemicals which are call phytochemicals. These phytochemicals exhibit several biological activities. Every day we take lots of phytochemicals with foods. These phytochemicals regulate our body systems. In present investigation, the leaves methanolic extract of R. madagascariensis was subjected to the Preliminary phytochemicals screening. This investigation revealed that the presence of various potential phytochemicals such as tannins, saponins, steroids, terpenoids as well as triterpenoids. The presence of these phytoconstituent exhibit potential biological activities like as analgesic, cardioprotective, Lipid lowering activity, antidiabetics, hepatoprotective, antidiarrhoeal, anticancer, antiasthmatic activities, antioxidant, antimicrobial and so on. These investigation only preliminary studies to isolate potential compounds which may be use as a lead compound for several biological activities. Further depth investigation required to find out lead compounds. - See more at: http://www.wjpsonline.org/view_issue.php?title=Potential-in-vitro-phyto-chemicals-investigation-of-leaves-of-Ravenala-madagascariensis-sonnerat#sthash.9Rf6I3Y4.dpuf

A rapid and precise high performance liquid chromatography method has been developed for the validation of Salmeterol xinofoate in its pure dosage form. The separation was carried out on Agilent Zorbax Bonus RP-(250mm ×4.6mm 5µ) column with a mobile phase consisting of 0.1% Formic acid: Acetonitrile in the ratio of 64:36 v/v as a mobile phase and flow rate is 1ml/min. The detection was carried out at wavelength 234nm. The column thermostatically controlled at 30℃. The retention time of Salmeterol was found to be 1.96 min. The Salmeterol xinofoate followed linearity in the concentration range of 40-60µg/mL with r 2 = 0.999. The developed method was validated for sensitivity, accuracy and precision. The sample was scanned from 200-400nm with PDA detector. The % recovery of sample was found to be. The LOD and LOQ of the Salmeterol xinofoate was found to be 2.67µg/ml and 8.08µg/ml respectively. The suitability of this HPLC method for quantitative estimation of Salmeterol xinofoate was p...

Diabetic retinopathy (DR), commonly classified as a microvascular complication of diabetes, is now recognized as a neurovascular complication or sensory neuropathy resulting from disruption of the neurovascular unit. Current therapies for DR target the vascular complication of the disease process, including neovascularization and diabetic macular edema. Since neurodegeneration is an early event in the pathogenesis of DR, it will be important to unravel the mechanisms that contribute to neuroretinal cell death in order to develop novel treatments for the early stages of DR. In this review we comment on how inflammation, the metabolic derangements associated with diabetes, loss of neuroprotective factors, and dysregulated glutamate metabolism may contribute to retinal neurodegeneration during diabetes. Promising potential therapies based on these specific aspects of DR pathophysiology are also discussed. Finally, we stress the importance of developing and validating new markers of visual function that can be used to shorten the duration of clinical trials and accelerate the delivery of novel treatments for DR to the public.

3-benzoil-1-feniltiourea telah disintesis melalui reaksi asilasi antara senyawa benzoil klorida dengan senyawa 1-feniltiourea menggunakan pelarut tetrahidrofuran dan katalis trietilamin dengan cara refluks dan pengadukan selama 6 jam. Persentase hasil sintesis yang diperoleh adalah 89 %. Kemurnian hasil sintesis ditunjukkan dengan adanya noda tunggal pada KLT dan jarak lebur yang sempit. Hasil identifikasi struktur dengan spektrofotometri UV, spektroskopi infra merah, spektroskopi 1HNMR dan spektroskopi massa menunjukkan struktur senyawa hasil sintesis sesuai dengan yang diperkirakan. Studi interaksi secara in silico menggunakan program Autodock Vina dan MMV menunjukkan senyawa 3-benzoil-1-feniltiourea memiliki interaksi yang baik terhadap reseptor kanker paru-paru (2ITO) melalui ikatan hidrogen dengan residu-residu asam amino yaitu Ala 839, Asn 842 dan Lys 852 dan dengan nilai energi afinitas -6,5 kkal/mol.

Organophosphate (OP) pesticides and nerve agents are responsible for suicidal and accidental poisonings. The acute toxicity of nerve agents leads to progressive inhibition of the enzyme acetylcholinesterase (AChE) by phosphylation of serine residue at the active site of gorge. The recent massive destruction of Syrian civilians by nerve gas sarin, has again renewed the research attention of global science fraternity towards nerve agents, their mode of action and most prominently their therapeutic treatment. This review is principally focused on nerve agent intoxication. The common approach to deal with OP-intoxication is, application of antimuscarinic drug (atropine), anticonvulsant drug (diazepam) and clinically used oximes (pralidoxime, trimedoxime, obidoxime and asoxime). However, the existing therapeutic approach is arguable and has several failings to cure all kinds of nerve agent poisonings. Considering this issue, numerous oximes have been synthesized and screened through various in-vitro and in-vivo studies in last decade to overcome the downsides. At present, only a few oximes (bis pyridinum-oximes) exhibit sound efficacy against selective OPs. In spite of extensive efforts, till date no oxime is available as a universal antidote against all the classes of OPs. This review is centered on the recent developments and structural modification of AChE reactivators against nerve agent toxicity. In particular, a deeper look has been taken into chemical modifications of the reactivators by incorporation of different structural moieties targeted towards the increased reactivation affinity and improved blood brain barrier (BBB) penetration.

Although vaccines and antibiotics could kill or inhibit microbes, many infectious diseases remain difficult to treat because of acquired resistance and adverse side effects. Nano-carriers-based technology has made significant progress for a long time and is introducing a new paradigm in drug delivery. However, it still has some challenges like lack of specificity toward targeting the infectious site. Nanocarriers utilized targeting ligands on their surface called ‘active target’ provide the promising way to solve the problems like accelerating drug delivery to infectious areas and preventing toxicity or sideeffects. In this mini review, we demonstrate the recent studies using the active targeted strategy to kill or inhibit microbes. The four common nano-carriers (e.g. liposomes, nanoparticles, dendrimers and carbon nanotubes) delivering encapsulated drugs are introduced.

Abstract
Ayurvedic medicinal preparation as per Ayurveda by using herbal antioxidant ingredients; the name of prepared formulation in Ayurveda is called churna, That churna having antioxidant property known to be effective in all types of allied disorders also, related to oxidation in cellular and molecular level in a living system has been standardized by following modern scientific quality control procedures both for the raw material and finished product. The obtained values of physical and chemical parameters can be adopted to lay down new pharmacopoeia standards to be followed for traditional preparations of antioxidant churna with batch-to-batch consistency. The Physicochemical constituents found to be present in the raw material used the preparation of antioxidant churna possible facilitate the desirable therapeutic efficacy of the medicinal formulation, and also could help in knowing the underlying mechanisms of Pharmacological Action.
Keywords: Standardization, Antioxidant Churna, Ayurvedic Polyherbal formulation, Pharmacopoeia standards.

A novel series of 4-[2-(3-bromophenyl)-7-nitro-4-oxo-3,4-dihydro-3-quinazolinyl]benzoyl amino acids and di/tripeptides was synthesized using diisopropylcarbodiimide (DIPC) as the coupling agent and N-methylmorpholine (NMM) as the base. Structures of all the newly synthesized peptide analogs were elucidated using IR, 1H/13C NMR, MS spectral data and evaluated for antimicrobial potential against pathogenic microbes. Most of the compounds exhibited potent antifungal activity against pathogenic Candida albicans and dermatophytes, in comparison to reference compound. Good bioactivity was also seen against gram-negative bacteria for synthesized compounds.

Objective: The main objective of this research work was to synthesis the triazoles compounds by Click reaction and
evaluated their antibacterial activities against gram positive and gram negative bacteria. Material and Methods: In
this work 1,4-disubstituted 1,2,3-triazole compounds (3a-3i) were synthesized by Azide Alkyne Cycloaddition
reaction and characterized by IR, H NMR and Mass spectroscopy. Further these compounds were evaluated for 1
antibacterial activity against Bacillus substilus, Staphylococcus aureus and Escherichia coli by using Ciprofloxacin as
standard compound with various concentrations. Results: Among all the compounds (3a-3i) which were screened for
antibacterial activity, the compounds 3c, 3d, 3e and 3i were found to be excellent antibacterial agents. Conclusion:The
presence of electron donating, electron withdrawing and halogen groups plays an important role of biological activity
of compounds.

The aim of our current research was to synthesize some transition metal complexes of Naproxen, determine their physical properties, and examine their relative stability under various conditions. Characterizations of these complexes were done by 1H-NMR, Differential Scanning Calorimetry (DSC), FT-IR, HPLC, and scanning electron microscope (SEM). Complexes were subjected to acidic, basic, and aqueous hydrolysis as well as oxidation, reduction, and thermal degradation. Also the reversed phase high-performance liquid chromatography (RP-HPLC) method of Naproxen outlined in USP was verified for the Naproxen-metal complexes, with respect to accuracy, precision, solution stability, robustness, and system suitability. The melting points of the complexes were higher than that of the parent drug molecule suggesting their thermal stability. In forced degradation study, complexes were found more stable than the Naproxen itself in all conditions: acidic, basic, oxidation, and reduction media. All the HPLC verification parameters were found within the acceptable value. Therefore, it can be concluded from the study that the metal complexes of Naproxen can be more stable drug entity and offer better efficacy and longer shelf life than the parent Naproxen.

ABSTRAK
Penelitian isolasi dan uji aktivitas antibakteri dari sumber Spons laut (Plakortis simplex) yang berasal dari perairan selatan Gunungkidul telah dilakukan. Penelitian ini bertujuan untuk mengisolasi senyawa antibakteri yang berasal dari spons laut (Plakortis simplex) dan melakukan uji antibakteri terhadap bakteri Escherichia coli dan Staphylococcus aureus menggunakan metode difusi agar.
Isolasi dilakukan dengan maserasi menggunakan campuran metanol:diklorometana (3:2 v/v). Ekstrak diklorometana kemudian dipekatkan dan dipartisi dalam etil asetat:air (1:1 v/v). Ekstrak etil asetat diambil dan diuapkan sehingga diperoleh ekstrak kasar kemudian dipisahkan dengan kromatografi kolom dengan eluen berturut-turut dari n-heksana hingga metanol. Ekstrak kasar diuji toksisitasnya menggunakan metode Brine Shrimp Lethality Test (BSLT). Pengujian antibakteri setiap fraksi menggunakan metode difusi agar terhadap bakteri E coli dan S aureus. Fraksi yang mengandung senyawa aktif dianalisis menggunakan Liquid Chromatography-Mass Spectrometry (LC-MS).
Hasil ekstraksi diperoleh 0,534 g ekstrak kasar  berwarna cokelat kehijauan dan berbau menyengat. Uji BSLT memberikan nilai Lethal Concentration 50% (LC50) 140,96 ppm. Pemisahan kromatografi kolom diperoleh 6 fraksi pemisahan dengan fraksi 3 diuji antibakteri dan analisis menggunakan LC-MS. Hasil uji terhadap bakteri E. coli dan S. Aureus menunjukkan aktivitas penghambatan yang kuat pada konsentrasi 250 ppm hingga 500 ppm. Hasil analisis LCMS terhadap fraksi 3 diperkirakan senyawa 9,10-dihidroplakortin, plakortin, dan plakortida G.

Kata kunci : Antibakteri, Plakortis simplex, Escherichia coli, Staphylococcus aureus, Metode difusi agar

The problem of anemia in most rural communities in Nigeria is enormous especially among children and pregnant women. Therefore, communities tend to explore alternative and cheaper means in treating anaemic disease condition when they occur. The study was carried out to test for the haematoprotective property of ethanol extract of Eremomastax speciosa (Hocht.) Acanthaceae leaves. Phenylhydrazine was used to induce anaemia by intraperitoneal injection. Two doses of the extract (300 and 500 mg/Kg body weight) were administered to the anaemic test groups by oral gavage. The control groups (normal and anaemic) were given normal saline instead of the extract. All the experimental animals had access to distilled water and rat chow ad libitum. The effect of the extract was tested on haematological indices of the experimental animals. Result: the results showed that there were significant (P< 0.05) increases in the haemoglobin, red blood cell count, and haematocrit, when compared with the...

A series of new 4-aryl-8-arylidene-2-imino-5,6-dihydro-4H,7H-(3,1) benzothiazines , with an
aim to obtain potent Anti-tubercular agents. There were synthesized of Cyclohexanone of
Claisen - Schmidt Condensation and Aldol Condensation with various aromatic and
heterocyclic Aldehydes in presence of dilute sodium hydroxide gives the corresponding 2,6-
diarylidine Cyclohexanones step(1). Further these compounds of step 1 were subjected to
cyclocondensation with thiourea catalysed by aqueous Pottasium hydroxide to form 4-aryl-
8arylidene-2-imino-5,6-dihydro 4Hydrogen,7Hydrogen-(3,1) benzothiazines. The structure of
synthesized compounds, were characterized by their spectral studies and the anti-tuburcular
activity of these compounds is studied on Mycobacterium tuberculosis(H37 RV strain)
Key words: Benzothiazines, mycobacterium tuberculosis strain. Hetero cyclic aldehydes and
aromatic aldehydes

The term ribosome-inactivating protein (RIP) is used to denominate proteins mostly of plant origin, which have N-glycosidase enzymatic activity leading to a complete destruction of the ribosomal function. The discovery of the RIPs was almost a century ago, but their usage has seen transition only in the last four decades. With the advent of antibody therapy, the RIPs have been a subject of extensive research especially in targeted tumor therapies, which is the primary focus of this review. In the present work we enumerate 250 RIPs, which have been identified so far. An attempt has been made to identify all the RIPs that have been used for the construction of immunotoxins, which are conjugates or fusion proteins of an antibody or ligand with a toxin. The data from 1960 onwards is reviewed in this paper and an extensive list of more than 450 immunotoxins is reported. The clinical reach of tumor-targeted toxins has been identified and detailed in the work as well. While there is a lot of potential that RIPs embrace for targeted tumor therapies, the success in preclinical and clinical evaluations has been limited mainly because of their inability to escape the endo/lysosomal degradation. Various strategies that can increase the efficacy and lower the required dose for targeted toxins have been compiled in this article. It is plausible that with the advancements in platform technologies or improved endosomal escape the usage of tumor targeted RIPs would see the daylight of clinical success.

Context: Nicotiana tabacum is an herbaceous plant mostly known as tobacco. Locally, people do extract this plant with cow urine, they call it "Adimenu" and they claimed it is effective in managing various ailments, even with taking just a spoonful of the extract. Thus, profiling the toxicity and or otherwise of the cow-urine extracted tobacco plant cannot be overemphasized. Aims: To characterize the cow urine extracts of N. tabacum and evaluated the sub-acute toxicity of smokeless exposure in male Wistar rats. Methods: Forty male Wistar rats were randomly assigned into groups and exposed to different doses (50, 100 and 200 mg/kg body weight) of N. tabacum extract for 7 and 28 days, after which the animals were sacrificed for the biochemical assays. Results: The GC-MS analysis revealed 21 compounds in the N. tabacum extract. As expected, nicotine was predominant among the identified compounds. The sub-acute exposure of rats to cow-urine extract of N. tabacum extract might have altered rat metabolic homeostasis, triggering adaptive mechanisms, while impairing renal functions. The N. tabacum extract also modulated (p<0.05) rat serum lipid profile when compared with control. Conclusions: Findings in this study suggest that the cow-urine extract of N. tabacum exposure in male Wistar rats might have perturbed rat renal functions as well as modulated serum lipid profile. This research, therefore, recommends to local consumers to be cautious of the rate at which they consume their regular "Adimenu".

The World Health Organization has reported about 214 million new cases of malaria with about 438,000 deaths worldwide in 2015. An example of antimalarial compounds isolated from plants, and is currently in use, may be mentioned quinine and artemisinin. However, one of the major problems that have arisen in recent years is the resistance of parasites against existing antimalarial drugs. Thus, there is a strong need to find new agents to control and to eradicate the disease. In this regard, marine organisms constitute a universally recognized source of potentially bioactive molecules, which have been enzymatically engineered and biologically validated. In this study, a quantitative structure–activity relationship (QSAR) analysis has been performed on data set of 14 bromopyrrole alka-loids (sponge metabolites) for antimalarial activity. Using density functional theory (DFT) several types of descriptors, including thermodynamics and electronic, have been calculated , in order to derive a quantitative relationship between antimalarial activity and structural properties. Simple and multiple regressions were used to generate the model. The best model (r 2 = 0.97, Q 2 = 0.86, F = 41.85) was obtained with descriptors as entropy, dipole momentum , molecular polarizability, HOMO energy softness, and electrophilic Index. The robustness of the QSAR models was verified by the leave-one-out cross-validation and external validation methods. The model obtained in this study should aid further study and could suggest some characteristics of novel potent bromopyrrole alkaloids against malaria.

Ashwagandha (Withania somnifera) is a one of the most important and reputed Indian traditional medicinal plant. Multiple shoot in vitro culture of Ashwagandha plants in two nutrient basal medium (i.e.in MS and B5 basal medium) were experimental established by using nodal excised small segments as explants. The hormonal combinations and mixture of BAP, 2,4-D and NAA not only enhanced there in vitro morphogenetic response but also differentially increases the level of bio-generation or biological production of withanolide A through in vitro shoots formation in two basal nutrient medium. Withanolide-A, that was normally present in high quantity and high proportion in the aerial region and parts of Ashwagandha (explants source) which is propagated and grown in field and now it is proof that their concentration regularly increased in the in vitro shoot or stem cultures by nodal excised segments of the Withania somnifera plant. The productivity and isolation of withanolide-A in the in vitro cultures varied and fluctuates between 0.014-0.14 mg/gram of fresh weight of Withania plant with the alternatively change in the growth hormone composition and concentration of the nutrient culture basal media as well as its genotype used as important source of the excised explants.

Systems thinking has become an essential part of modern medicinal chemistry and new drug development. It is based on
the concepts that complex problems almost always have multiple causes and that there are often connections that have not
always been obvious. In contrast to reductionist thinking, systems thinking uses network theory and nonlinear mathematics
to prevent, diagnose, treat and even cure diseases. Systems thinking is an integral part of predictive, preventive, personalized
and participatory (P4) medicine. It takes not just a holistic but also a quantitative and mathematical approach to practicing
medicine. This includes using networks of professionals. That is, in the 21st century doctors, mathematicians, physicists,
chemists, biologists, systems engineers and many others have been working together to develop new pharmaceutical compounds
and medicines. Modern drug development is being done through collaborative initiatives between governments,
universities, research institutes, hospitals and industry. The U.S. Food and Drug Administration (FDA) has a Critical Path
Initiative that intends to modernize drug development by incorporating recent scientific advances, such as genomics and
advanced imaging techniques into the process of developing new drugs and medicines. There are also Biomarker-Integrated
Approaches for Targeted Therapy for Lung Cancer Elimination (BATTLE) and a Cancer Genome Anatomy Project (CGAP).
The National Cancer Institute (NCI) also has a Cancer Genomics’ Cancer Genome Characterization Initiative, or CGCI. Together,
these efforts are ushering in a new era of personalized health care that will be able to prevent, diagnose and properly
treat diseases with the help of patients and their caregivers.

Cancer has become a serious concern in public health. Harmful side effects and multidrug resistance of traditional chemotherapy have prompted urgent needs for novel anticancer drugs or therapeutic approaches. Anticancer peptides (ACPs) have become promising molecules for novel anticancer agents because of their unique mechanism and several extraordinary properties. Most α-helical ACPs target the cell membrane, and interactions between ACPs and cell membrane components are believed to be the key factor in the selective killing of cancer cells. In this review, we focus on the exploitation of the structure and function of α-helical ACPs, including the distinction between cancer and normal cells, the proposed anticancer mechanisms, and the influence of physicochemical parameters of α-helical ACPs on the biological activities and selectivity against cancer cells. In addition, the design and modification methods to optimize the cell selectivity of α-helical ACPs are considered. Furthermore, the suitability of ACPs as cancer therapeutics is discussed.

BACKGROUND AND PURPOSE
Methcathinone (MCAT) is a potent monoamine releaser and parent compound to emerging drugs of abuse including mephedrone (4-CH3 MCAT), the para-methyl analogue of MCAT. This study examined quantitative structure–activity relationships (QSAR) for MCAT and six para-substituted MCAT analogues on (a) in vitro potency to promote monoamine release via dopamine and serotonin transporters (DAT and SERT, respectively), and (b) in vivo modulation of intracranial self-stimulation (ICSS), a behavioural procedure used to evaluate abuse potential. Neurochemical and behavioural effects were correlated with steric (Es), electronic (σp) and lipophilic (πp) parameters of the para substituents.
EXPERIMENTAL APPROACH
For neurochemical studies, drug effects on monoamine release through DAT and SERT were evaluated in rat brain
synaptosomes. For behavioural studies, drug effects were tested in male Sprague-Dawley rats implanted with electrodes targeting the medial forebrain bundle and trained to lever-press for electrical brain stimulation.
KEY RESULTS
MCAT and all six para-substituted analogues increased monoamine release via DAT and SERT and dose- and time-dependently modulated ICSS. In vitro selectivity for DAT versus SERT correlated with in vivo efficacy to produce abuse-related ICSS facilitation. In addition, the Es values of the para substituents correlated with both selectivity for DAT versus SERT and magnitude of ICSS facilitation.

Context: Azadirachta indica has long been used in herbal or folk medicine as a remedy for the treatment of malaria and the administration of herbal preparations has raised concerns on their toxicity. Aims: To determine the phytochemical content of A. indica and its therapeutic effect on indices of clinical importance in malaria-induced male Wistar rats. Methods: Plant material was extracted with ethanol, and the lethal dose (LD50) on the rats was determined before the study. Normal and Plasmodium berghei infected rats were divided into eight groups of five rats each with groups 1 and 2 serving as normal and disease control respectively. Lumartem was administered twice daily at oral therapeutic doses of artemether/lumefantrine (2/12 mg/kg) and plant extract at 300 and 500 mg/kg body weight. After 5 days of treatment, all the animals were sacrificed according to their groups for the experimental analysis. Results: The plant extract was considered safe with LD50 &gt; 5000 mg/kg body we...

he basic composition (The total protein, total carbohydrate, total lipid, crude fiber and ash content of each mushroom were studied on dry weight contents were determined in the cultivated mushrooms Agaricus bisporus/ white, Agaricus bisporus/brown, Lentinula edodes, and Pleurotus ostreatus and they ranged from 28.38-49.2, 1.54- 4.96, 13.2-29.02 and 7.01-17.92, respectively. This study suggested that cultivated mushrooms were in rich of protein and fiber with low fat content. Hence these nutrients contents made mushroom as a low energy, healthy foodstuff and these mushrooms may also be used as protein supplementary diet.

Aspartic peptidases are proteolytic enzymes present in many organisms like vertebrates, plants, fungi, protozoa and in some retroviruses such as human immunodeficiency virus (HIV). These enzymes are involved in important metabolic processes in microorganisms/virus and play major roles in infectious diseases. Although few studies have been performed in order to identify and characterize aspartic peptidase in trypanosomatids, which include the etiologic agents of leishmaniasis, Chagas’ disease and sleeping sickness, some beneficial properties of aspartic peptidase inhibitors have been described on fundamental biological events of these pathogenic agents. In this context, aspartic peptidase inhibitors (PIs) used in the current chemotherapy against HIV (e.g., amprenavir, indinavir, lopinavir, nelfinavir, ritonavir and saquinavir) were able to inhibit the aspartic peptidase activity produced by different species of Leishmania. Moreover, the treatment of Leishmania promastigotes with HIV PIs induced several perturbations on the parasite homeostasis, including loss of the motility and arrest of proliferation/growth. The HIV PIs also induced an increase in the level of reactive oxygen species and the appearance of irreversible morphological alterations, triggering parasite death pathways such as programed cell death (apoptosis) and uncontrolled autophagy. The blockage of physiological parasite events as well as the induction of death pathways culminated in its incapacity to adhere, survive and escape of phagocytic cells. Collectively, these results support the data showing that parasites treated with HIV PIs have a significant reduction in the ability to cause in vivo infection. Similarly, the treatment of Trypanosoma cruzi cells with pepstatin A showed a significant inhibition on both aspartic peptidase activity and growth as well as promoted several and irreversible morphological changes. These studies indicate that aspartic peptidases can be promising targets in trypanosomatid cells and aspartic proteolytic inhibitors can be benefic chemotherapeutic agents against these human pathogenic microorganisms.

Thiourea is one of the compounds that are useful in studies of new drug discovery. Some thiourea derivatives have potent pharmacological activity as anticancer [1-9].
1-benzoyl-3–Phenylthiourea compound has been synthesized through acylation reaction between benzoyl chloride with 1-Phenylthiourea using tetrahydrofuran as solvent and triethylamine as catalyst by reflux and stirring for 6 hours . Synthesis results obtained percentage is 89 % . The purity of the synthesis results indicated the presence of a single stain on TLC and narrow melting range .
From the characterization by UV spectrophotometry , infrared spectroscopy, 1-HNMR spectroscopy and mass spectroscopy can be concluded that the resulting compound is 1-benzoyl-3- phenylthiourea structure. From the in vitro test obstained IC-50 of 1-benzoyl-3-phenyl thiourea on HeLa cells at 702 g/ml, and IC-50 on MCF-7 cells at 398 g/ml.

Pyrimidine derivatives are a group of heterocyclic compounds which are associated with a wide variety of biological activities. Broad spectrum of biological activities of pyrimidine derivatives elated to synthesize a series of some new different pyrimidine derivatives by condensation of different chalcones with guanidine hydrochloride in the presence of potassium hydroxide as catalyst. The synthesized pyrimidine derivatives were purified by either recrystallization or column chromatographic techniques. The characterization of the purified pyrimidine derivatives was done by IR, 1 H NMR spectral data and elemental analysis. These compounds were further screened for anti-inflammatory and cytotoxic activities using standard protocols. When these pyrimidine derivatives were evaluated for anti-inflammatory and cytotoxic activities some of them found to possess significant biological activity when compared to standard drugs.

A series of novel N-[6-fluoro-7-substituted-1,3-benzothiazol-2-yl]-4-[3-chloro-2-(3-nitrophenyl)-4-oxo-azetidin-1-yl]benzenesulfonamide 6-17 and N-[6-fluoro-7-substituted-1,3-benzothiazol-2-yl]-4-[3-chloro-2-(4-nitrophenyl)-4-oxo-azetidin-1-yl]benzenesulfonamide 18-29 derivatives were synthesized using appropriate synthetic route. Their structures were characterized by elemental analysis, UV, IR and 1 HNMR. The entire test compounds 6-29 were screened for anti-microbial activity which exhibited good to moderate activity.

Alkaline phosphatase (AP, EC 3.1.3.1.) is a metalloenzyme that belongs to a family of ectonucleotidases. The other members of ectonucleotidase family are ecto-nucleoside triphosphate diphosphohydrolases (E-NTPDases), ecto-nucleotide pyrophosphatase/phosphodiesterases (E-NPPs) and ecto-5ʹ-nucleotidase (e5ʹNT). These ectonucleotidases are responsible for hydrolyzing extracellular nucleotides to nucleosides including adenosine. Many of these extracellular nucleotides and adenosine are important signaling molecules that act on their respective receptors (adenosine activated P1 receptor; nucleotide activated P2 receptor, each having many sub-types) and are therefore responsible for triggering cellular responses that lead to important physiological and immunological changes. A dedicated, concerted cohort of ectonucleotidases is responsible for controlling the availability of these extracellular signaling molecules at their respective receptors. Inhibitors of these ectonucleotidases provide the means by which these cellular processes can be modulated. This mini review has been written in the wake of mounting evidence of potential therapeutic benefits associated with inhibition of alkaline phosphatases and aims to provide prolific leads to design more potent and selective AP inhibitors.

The integration of lipoprotein-related or apolipoprotein-targeted nanoparticles as pharmaceutical carriers opens new therapeutic and diagnostic avenues in nanomedicine. The concept is to exploit the intrinsic characteristics of lipoprotein particles as being the natural transporter of apolar lipids and fat in human circulation. Discrete lipoprotein assemblies and lipoprotein-based biomimetics offer a versatile nanoparticle platform that can be manipulated and tuned for specific medical applications. This article reviews the possibilities for constructing drug loaded, reconstituted or artificial lipoprotein particles. The advantages and limitations of lipoproteinbased delivery systems are critically evaluated and potential future challenges, especially concerning targeting specificity, concepts for lipoprotein rerouting and design of innovative lipoprotein mimetic particles using apolipoprotein sequences as targeting moieties are discussed. Finally, the review highlights potential medical applications for lipoprotein-based nanoparticle systems in the fields of cardiovascular research, cancer therapy, gene delivery and brain targeting focusing on representative examples from literature.

Quinazolines are the most important class of heterocyclic compounds. Quinazoline is a bicyclic compound
consisting of a pyrimidine system fused at 5, 6 with benzene ring Quinazoline is considered as an important
chemical synthesis of various physiological significance and pharmacological utility. Cancer is a disease
characterized by uncontrollable, irreversible, independent, autonomous, uncoordinated and relatively unlimited and
abnormal over growth of tissues. The drugs containing Quinazoline groups were the first effective chemotherapeutic
agents which were systematically proved for the prevention and cure of bacterial infection in human beings.
Literature revealed that Quinazoline derivatives may serve as an important model on as potent anti-cancer agent.
When one biological active molecule is linked to another, resultant molecule generally has increased potency. Most
of the derivatives showed enhanced anti-cancer activity. So, Quinazoline derivatives can serve as future therapeutic
leads for the discovery of anti-cancer drugs. This review was focused on the Quinazolines and its different
derivatives that posses anticancer activities.
Keywords: Quinazolines, Cancer, Cytotoxic Activity, Antiproliferative Activity, Antitumor activity

Monoamine oxidase (MAO) A and B are flavin adenine dinucleotide (FAD) containing enzymes which are tightly anchored to the mitochondrial outer membrane. MAO-A inhibitors are particularly effective in the treatment of depression in elderly patients and inhibitors of MAO-B are employed in the treatment of neurodegenerative disorders such as Parkinson’s disease (PD).1 The docking protocols to virtually screen selective monoamine oxidase B (MAO-B) ligands using PLANTS docking software were developed and  validated. Binding of 2-(2-benzofuranyl)-2-imidazoline (XCG) to monoamine oxidase B (MAO-B) was used as the model for study. The results showed that developed protocols could predict the binding pose of  XCG  to MAO-B accurately (RMSD = 1.0069 Ǻ).