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

Annals of the Romanian Society for Cell Biology

Derivatization: Tool In Analytical Separations Of Compound

The present work describes biological evaluation of target molecules designed by molecular docking with 4h1j protein using Autodock Vina docker. Designed novel benzothiazole and coumarin based 6-(3, 5-dimethylpyrazol-1-yl) pyridazin-3-one derivatives were synthesized by condensation of substituted 6-(3,5-dimethylpyrazol-1-yl)pyridazin-3(2H)-one with substituted 2-amino benzothiazoles, substituted 2-oxo-2H-chromene-3-carbonyl chloride or 4-(bromomethyl)-2H-chromen-2-one. Synthesized compounds were characterized by spectral analysis and screened for antioxidant activity using 1, 1-diphenyl-2-picrylhyrazyl radical scavenging, Hydrogen peroxide scavenging and ferric reducing antioxidant power method. The compounds 5c and 9b showed more antioxidant potential and other compounds showed moderate to less activity as compared to standard Ascorbic acid and Butylated hydroxyl toluene.

Research Journal of Pharmacy and Technology

Design, synthesis, characterization and antioxidant activity of novel benzothiazole and coumarin based 6-(3, 5-dimethylpyrazol-1-yl) pyridazin-3-one derivatives

A new series of N-(benzo[d]thiazol-2-yl)-[1,2,4]triazolo[4,3-c]quinazoline-5-carboxamide derivatives were synthesized by condensation of [1,2,4]triazolo[4,3-c]quinazoline-5-carboxylate derivatives with substituted benzothiazoles. The chemical structures of the synthesized compounds were confirmed by FT-IR, MS and 1H NMR spectra. Designed triazoloquinazoline derivatives were docked with oxido-reductase enzyme (PDB Code 4h1j) and DNA gyrase enzyme (PDB Code 3g75). Based on high binding affinity score, the best compound were selected for synthesis and subjected to in vitro antioxidant and antibacterial activity. Compounds 7a and 7d were found to be most active compounds as antioxidant agent among this series when compared with ascorbic acid. Compounds 7a, 7d and 7f were found to be most active compounds as an antibacterial agents among this series when compared with ciprofloxacin against bacterial strains such as S. aureus (ATCC 25923), E. coli (ATCC 25922) and P. aeruginosa (ATCC 27853). Study revealed that the most active compounds after structural modifications can be exploited as lead molecules for other pharmacological activities such as anti-inflammatory, anticancer and antidepressant activities.

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Asian Journal of Chemistry

Design, Synthesis and Biological Evaluation of Novel Benzothiazole Based [1,2,4]Triazolo[4,3-c]quinazoline Derivatives

Quinoxaline, triazole and benzothiazole heterocycles plays an important role in modulating biological activity. The present work describes the biological evaluation of target molecules designed using autodock vina docker. Novel benzothiazole based [1, 2, 4]-triazolo [4, 3-a] quinoxalines were synthesized by condensation of substituted 2-amino benzothiazoles and 4-chloro triazoloquinoxalines. The synthesized compounds were characterized by analysis of physical and spectral data. All synthesized compounds were screened for antioxidant activity using 1, 1-Diphenyl-2-picrylhyrazyl radical scavenging, Hydrogen peroxide scavenging and Ferric reducing antioxidant power Method. The compounds 10g and 10i were found to be most active compounds of this series and other compounds showed moderate to less activity when compared with ascorbic acid. Study revealed that the most active compounds after structural modifications can be exploited as lead molecules for other pharmacological activities such as antimicrobial, anti-inflammatory, anticancer and antidepressant, activity.

Design, synthesis, characterization and biological evaluation of novel benzothiazole based [1, 2, 4]-triazolo [4, 3-A] quinoxaline derivatives

Objective: The present work describes stability indicating (SI) RP-HPLC-PDA method for determination of abiraterone acetate (ABA) and characterization of its base catalyzed degradation product by LC-MS. Methods: The separation was achieved by using column Kromasil C18 (250 mm x 4.6 mm, 4.0 µ) using acetonitrile (ACN): ammonium acetate buffer 10 mM, pH adjusted to 3.5 with acetic acid (AA) in the ratio of 10:90 % v/v as eluent. The Mobile phase flow rate was 0.6 ml/min and data integration was achieved at 235 nm. Results: The retention time of ABA was 5.4±0.01 min. Linearity was found to be in the range of 5-30 µg/ml. The limit of detection and quantitation were 0.25 µg/ml and 0.75 µg/ml respectively and percentage recovery of ABA was found to be 99.52 to 100.13 %. Mass spectral data of base degraded product of ABA shows a prominent molecular ion peak at m/z-391.5. Major fragmentation leads to formation of 10-Methyl 2,3,4,7,8,9,10,11,12,13,14,15-dodecanhydro-1H cyclopenta (a)phenanthren-3-ol as a degradant (D2) at m/z-257.81, due to corresponding loss of C8H12ON. All the analytical validation parameters were determined and found in the limit as per ICH guidelines. Conclusion: The results of the various validation studies showed that the LC method is fast, specific, accurate, reproducible, possessed significant linearity and precision. The drug was found to be stable under all the stress conditions except basic stress. Thus developed method reported first time is novel with a very short run time of 6 min..

International Journal of Pharmacy and Pharmaceutical Sciences

Stability indicating RP-HPLC-PDA method for determination of abiraterone acetate and characterization of its base catalyzed degradation product by LC-MS