Antioxidants exert their action chiefly in controlling and preventing the free-radicals and their reactions and thus it has a vital role as health protecting factor. There are many scientific data proposing that antioxidants lower the threats of some chronic diseases including cancer and heart disease. In the present work, the hybrid molecule i.e benzothiazole substituted 4-thiazolidinone, has been taken for the study and different novel benzothiazole substituted 4-thiazolidinone derivatives were synthesized by reacting 2-amino-6-methyl benzothiazole with aromatic aldehydes in alcohol media. The resulting Schiff bases were made to react with thioglycolic acid in dioxane. Characterization of synthesized compounds was done by IR, 1 H NMR and Mass spectroscopy. The same reaction was performed in the microwave assisted reaction condition and compared with conventional synthesis. In vitro antioxidant activities of compounds were performed by three different methods, out of which Compound TZ4 emerged as a promising molecule.

Background: Asiatic acid (AA) is a naturally occurring triterpenoid derivative of Centella asiatica (CA) with neuroprotective effect. The study aimed to design an ideal oral drug delivery system to treat Alzheimer's disease (AD) and develop chitosan-embedded liposomes comprising an extract of CA (CLCAE) and compare them with the chitosan-coated liposomes of asiatic acid (CLAA) for oral delivery to treat the initial phases of AD.  Methods: The solvent evaporation technique was used to develop CLCAE and CLAA, optimised with the experiment's design, and was further evaluated. Results: Nuclear magnetic resonance (NMR) studies confirmed coating with chitosan. Transmission electron microscopy (TEM) and atomic force microscopy (AFM) indicated the successful formation of CLCAE and CLAA. Differential scanning colorimetry (DSC) confirmed the drug-phospholipid complex. Furthermore, the rate of in vitro release of CLCAE and CLAA was found to be 69.43±0.3 % and 85.3±0.3 %, respectively, in 24 h. Ex vivo permeation of CLCAE and CLAA was found to be 48±0.3 % and 78±0.3 %, respectively. In the Alcl3-induced AD model in rats, disease progression was confirmed by Y-maze, the preliminary histopathology evaluation showed significantly higher efficacy of the prepared liposomes (CLCAE and CLAA) compared to the Centella asiatica extract (CAE) and they were found to have equivalent efficacy to the standard drug (rivastigmine tartrate). The considerable increase in pharmacodynamic parameters in terms of neuronal count in the CLAA group indicated the protective role against Alcl3 toxicity and was also confirmed by assessing acetylcholine (Ach) levels. The pharmacokinetic study, such as Cmax, Tmax, and area under curve (AUC) parameters, proved an increase in AA bioavailability in the form of CLAA compared to the pure AA and CLCAE forms. Conclusion: The preclinical study suggested that CLAA was found to have better stability and an ideal oral drug delivery system to treat AD.

Cancer, seen as one of the highly prevelant life endangering diseases today, is mainly associated with the lifestyle led by the population at risk. The superficial observation seen in cancer is the uncontrollable growth and dispersion of abnormal cells. Statistically, the number of patients who receive chemotherapy has been soaring high, which has drawn attention towards development of more reliable and less toxic cytotoxic agents. In the present work, hybrid structure of pyridopyrimidine substituted with pyrazole and triazine in individual turns is studied. Pyridopyrimidines are ortho fused bicyclic heterocyclic structures constituted by the amalgam of a pyridine and a pyrimidine ring. In silico studies with molecular docking was performed to filter best compounds out the 16 different derivatives. Most of the compounds showed satisfactory results for the in silico screening. In case of docking, among all the screened compounds, 1d, 1o, 2d and 2j showed best affinity towards 2EUF while 1n, 1o, 2g and 2h showed best binding towards 5FWK. On that account, these compounds may have a potential cytotoxic effect and hence could be utilized for further studies and explorations of their properties.

Background: Free radicals and ROS which are formed in normal physiological conditions, damages the cells if it is not eliminated by endogenous system which causes oxidative stress. Pyridopyrimidines are important molecule in heterocyclic chemistry, gaining interest because of their biological and pharmacological activities, especially for their potential anti-tumor, antibacterial and tyrosine kinase inhibitors, among other pharmacological properties along with anti-oxidant properties. Materials and Methods: In the current study, novel pyridopyrimidines derivatives i.e different substituted 7-phenyl-5-(thiophen-2-yl)-2-thioxo-2,3-dihydropyrido[2,3-d]pyrimidine-4(1H)-one(3a-p) were synthesized to develop potent anti-oxidant agent. Based the in-silico studies, especially depending on the docking score, 8 compounds were selected for the synthesis and evaluated for their anti-oxidant potency. Selected compounds were synthesized using mercapto-4hydroxy-6-amino pyrimidine (1) and substituted α, βunsaturated ketones(2a-p). Results: Synthesized compounds were characterized by IR, NMR and Mass spectra. In-vitro antioxidant studies were performed for 8 best scored compounds by DPPH assay and nitric oxide inhibition assay. From the in-vitro result, compound 3j, 3a, and 3o are considered as promising molecules. Conclusion: The promising activity may be because of presence of electron releasing group (3a-p-OH, 3o-p-NH 2 ) and electron withdrawing group (3jp-CF 3 ) which can be considered as lead molecules for the further discovery.

Background: Diabetes mellitus is a pervasive illness worldwide with many progressively increasing complications day by day. The quinoline nucleus is important heterocyclic moiety with different biological activities. Due to their pivotal role in different biological processes they are well explored as therapeutic agents and some of them have exhibited antihyperglycemic activity. Different substituted pyrazoles have been accounted for their in vivo antidiabetic activity, but we concentrated to substituted pyrazoline derivatives in the quest for novel basic classes of medications inhibiting the action of the ATP-K + beta cell pancreatic membrane channel, prompting the release of insulin. Materials and Methods: In the present study, 1-(4-(7-Chloroquinolin-4-yl oxy) phenyl ethanone and 1-(4-(7-Chloroquinolin-4-yl amino) phenyl ethanone was synthesized by nucleophilic substitution of 4-Chloro of 4,7-dichloroquinoline with substituted 4-hydroxy acetophenone and 4-amino acetophenone in DMF and KOH respectively. The amino linked chalcones and oxo linked chalcones was synthesized by Clasein Schmidt condensation with different substituted aromatic aldehydes. Finally substituted pyrazolines (ACP1-ACP10) was synthesized upon cyclisation of oxo linked and amino linked chalcones with hydrazine hydrate. The structures of the final synthesized compounds were characterized by IR, 1 H NMR and mass spectra. Results: The final synthesized compounds were evaluated for their in vitro antidiabetic activity by alpha glucosidase inhibition assay. Most of the compounds showed good antidiabetic activity compared to the standard drug acarbose. Conclusion:In-vitro results revealed that a large number of synthesized compounds having good antidiabetic activity. So these compounds are found to be interesting lead molecules for further synthesis as antidiabetic agents.

The core pyridopyrimidines are gaining interest in organic and heterocyclic chemistry in recent days, as this scaffold acts as a building block because of its wide range of biological and pharmacological applications like anticancer, antimicrobial, fungicidal, antiviral, CNS, antibacterial, and anti-inflammatory properties. This review mainly emphasizes the evolution in anticancer properties of pyridopyrimidines since 2008 especially the method of synthesis and anticancer activity of synthesized compounds with reporting of active anticancer scaffolds. Important starting materials which are widely used for the synthesis are 2-thioxopyrimidine, ethyl 2-cyanoacetate, 2-amino-3-cyano-4-trifluoromethyl-6-phenyl-pyridine, 2-amino-4,6-disubstituted nicotinonitrile, 2-chloro-3-pyridine carboxylic acid, in which 2-thioxopyrimidine is found to be mostly employed in the synthesis. Pyridopyrimidines which are synthesized from different starting materials, in which the more active compounds are reported here which may help in further discovery/ development of novel molecules.

Chalcone is a simple chemical structure which is present in most of the naturally occurring substances. Many chalcone derivatives are synthesized by Claisen-Schmidt condensation reaction. It is a subject of great research opportunity due to numerous biological activities and convenient synthesis of chalcones. This study aims on synthesizing different α, β unsaturated ketones (chalcones) containing thiophene from thiophene-2-carbaxldehyde and different substituted acetophenones, further evaluating antibacterial activity of synthesized compounds. The synthesized compounds are characterized for their spectral study. From the antibacterial study it was observed that the compounds bearing electron withdrawing group, electron releasing group exhibited excellent to moderate antibacterial activity respectively. These results showed that chalcones incorporated with thiophene have better scopes for further development of the antimicrobial agents.

Background: Cancer is one of the leading diseases associated with the high degree of mortality. In current scenario chemotherapy is the major treatment for cancer and it still has few limitations. The continuous seek for highly effective and safe anticancer agents is the one of the major goal for medicinal chemists. Objectives: In the present work, the hybrid molecule i.e benzothiazole substituted 4-thiazolidinone has been synthesized and evaluated for anticancer activity. Methods: A series of novel benzothiazole substituted 4-thiazolidinone derivatives were synthesized by reacting 2-amino-6-methyl benzothiazole with aromatic aldehydes in alcoholic media, resulting schiff bases are made to react with thioglycolic acid in dioxane. Characterization of synthesized compounds were done by IR, 1 H NMR, Mass spectroscopy. In silico studies with molecular docking was performed for the synthesized derivatives by taking proteins from PDB i.e VEGFR-2 kinase and Human thymidylate synthase (PDB ID:2QU5 and 5HS3) as the targets. Results and Discussion: Based on the docking score, best four compounds were selected and screened for in-vitro anticancer activity. From the in-vitro data, finally one potential molecule was selected and evaluated for in-vivo cytotoxic activity. Conclusion: All 4 screened derivatives were found to show good cytotoxic activity, out of which P14 can be considered as promising molecule.