MIT-World Peace University (MIT-WPU) is a top educational institute located in Pune, India. It is recognized within&nbsp;UGC under Government of Maharashtra Act No. XXXV 2017.&nbsp;

It is part of the MIT group of institutions (established in 1983) which covers 10+ campuses across India and has more than 50,000+ students enrolled across various disciplines at a given point of time. The institute houses 15 schools ranging from Engineering &amp; Technology, Design, Pharmacy, Commerce, Governance among others. It offers undergraduate, postgraduate and PhD programs among different disciplines.&nbsp;

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MIT World Peace University

This research is focused on designing, synthesis and biological evaluation of a series of coumarin based benzothiazole derivatives. The ligands were identified by docking study for antioxidant and antibacterial potential using target proteins PDB:4H1J and PDB:3G75, respectively. The target molecules were synthesized as a series of substituted N-(benzothiazol-2-yl)-2-oxo-chromene-3-carboxamides (7a–h) by condensation of substituted benzo[d]thiazol-2-amines with in situ synthesized substituted 2-oxo-2H-chromene-3-carbonyl chlorides. Infrared spectroscopy and 1H- nuclear magnetic resonance spectra were used to characterize the synthesized molecules. In vitro antioxidant activity of compounds was evaluated by DPPH and H2O2 radical scavenging assays. Antibacterial potential of compounds was evaluated using well diffusion method against Staphylococcus aureus (ATCC 25923), Escherichia coli (ATCC 25922) and Pseudomonas aeruginosa (ATCC 27853). Among synthesized derivatives, 7a showed good antioxidant potential whereas 7f showed antibacterial activity, which might be employed as lead molecules for future investigation for respective activities. © 2022 Indian Drug Manufacturers' Association. All rights reserved.

World University root node

School of Pharmacy

Pharmacy

Indian Drugs

DESIGN, SYNTHESIS AND EVALUATION OF N-(BENZO[D]THIAZOL-2-YL)-2-OXO-2H-CHROMENE-3-CARBOXAMIDE DERIVATIVES AS POTENTIAL ANTIOXIDANT AND ANTIBACTERIAL AGENTS

The selective optimization of side activities (SOSA) approach appears to be a promising strategy for lead generation. In this approach old drugs are used to generate new hits or leads. The objective of SOSA is to prepare analogues of the hit molecule in order to transform the observed ``side activity{''} into the main effect and to strongly reduce or abolish the initial pharmacological activity. The idea of taking a molecule with a primary activity in humans and then enhancing a secondary effect through structural changes describes the most common implementation of SOSA. An advantage to starting a drug discovery program with molecules that have already been tested in humans is that those molecules have already satisfied many safety criteria. Such molecules also likely have favourable pharmacokinetic profiles. In the present review different successful examples of SOSA switches are summarized. We hope that the present review will be useful for scientists working in the area of drug design and discovery.

JOURNAL OF PHARMACEUTICAL RESEARCH INTERNATIONAL

Selective Optimization of Side Activities (SOSA) as an Efficient Approach for Generation of New Leads from Old Drugs

In the current trend various regulatory authorities like ICH, USFDA, Canadian Drug and Health Agency are emphasizing on the identification and quantitation of impurities in Active Pharmaceutical Ingredient's (API's) and it is now emerging as a mandatory requirement for the new drug application. Hence their level should be controlled and monitored. Thus a simple sensitive High performance thin layer chromatographic (HPTLC) method for estimation of Propyl thiouracil and its process related impurities has been developed. Propyl thiouracil and its impurities were separated and identified on silica Gel 60 F254TLC plates with Hexane: Acetone: Ethyl Acetate: Formic acid 6:4:1:0.5 (v/v) as mobile phase. The plates were developed to a distance of 8 cm and quantification was performed at $\lambda$ = 254 nm. The method was validated for linearity, accuracy, precision and robustness according to ICH guidelines. The calibration plots were linear in the range 2500-5625 and 50-112.5 ng/band for API and its three impurities respectively. Here recovery value for API and impurities were found to be in the range of 99.99 to 100.75 % with % RSD value always less than 2. Hence the developed method was found to be simple, sensitive, accurate and precise which can be used for propyl thiouracil impurity profile study and for routine analysis of propyl thiouracil from its dosage forms and for IPQC study during manufacturing of its formulations.

International Journal of Pharmaceutical Sciences Review and Research

A validated HPTLC method for determination of propyl thiouracil in the presence of its impurities

Impurity profiling has gained importance in modern pharmaceutical analysis due to the fact that an unidentified, potentially toxic impurity are hazardous to health and in order to increase the safety of drug therapy, impurities should be identified and determined by selective methods. Thus a simple sensitive high performance thin layer chromatographic (HPTLC) method for estimation of Strontium ranelate and its impurities has been developed. Strontium ranelate and its impurities were separated and identified on silica Gel 60 F254TLC plates with Acetonitrile: Methanol: Ethyl acetate: Formic acid 9:1:1:1 (v/v) as mobile phase. The quantification was performed at $\lambda$ = 320 nm. The method was validated for linearity, accuracy, precision and robustness according to ICH guidelines. The calibration plots were linear in the range 4000-9000 and 40-90 ng/band for API and its two impurities respectively. The developed method can be used as a quality control tool for Strontium ranelate impurity profile study.

International Journal of Pharma and Bio Sciences

Development and validation of a HPTLC method for determination of strontium ranelate in the presence of its impurities

Repaglinide is a widely used meglitinide class drug to treat diabetes. The current study describes degradation as per ICH guidelines (hydrolysis, photolysis, dry heat and oxidation) and optimized assay method. A simple stability indicating method has been developed for Repaglinide in bulk drug. The peak purity of the drug was observed. For HPTLC study Aluminium plates precoated with Silica Gel 60 F254 was the stationary phase and mobile phase consisted of methanol: toluene (2:8) and quantitation was done at the wavelength 242nm. The method was found to be simple, specific, precise and stability indicating. {\textcopyright} RJPT All right reserved.