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Mini-Reviews in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Research Article

Facile and Solvent-free Domino Synthesis of New Quinolidinyl-2,4- thiazolidinones: Antifungal Activity and Molecular Docking

Author(s): Dnyaneshwar D. Subhedar, Mubarak H. Shaikh, Santosh G. Tupe, Mukund V. Deshpande, Vijay M. Khedkar, Prakash C. Jha and Bapurao B. Shingate*

Volume 18, Issue 7, 2018

Page: [622 - 630] Pages: 9

DOI: 10.2174/1389557516666161226161152

Price: $65

Abstract

Objective: We have synthesized new quinolidinyl-thiazolidinones via Knoevenagel condensation- alkylation reaction, catalyzed by [Et3NH][HSO4]. The present approach offers several advantages such as higher yields, eco-friendly reaction condition and economic availability of the catalyst.

Method: The newly synthesized compounds were evaluated for their in vitro antifungal activity against six fungal strains. Some of the synthesized conjugates displayed good to moderate antifungal activity.

Conclusion: Again, the molecular docking study performed against the fungal sterol 14α-demethylase (CYP51) showed an excellent binding affinity towards the enzyme which could rationalize the promising antifungal activity portrayed by these derivatives and provides a platform for structure based drug design.

Keywords: Antifungal activity, ionic liquid, molecular docking, multicomponent reaction, 2, 4-thiazolidinones, solvent-free reaction.

Graphical Abstract


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