Synthesis, in silico and antifungal studies of novel thiophene analogues containing pyrazole ring

Al-Maqtari, Helmi M. and Jamalis, Joazaizulfazli and Subhash Chander and Sirat, Hasnah M. and Naveen, S. and Lokanath, N. K. and Bohari, Siti P. M. and Bhagwat, Deepak P. and Sankaranarayanan, M. (2018) Synthesis, in silico and antifungal studies of novel thiophene analogues containing pyrazole ring. Letters in Drug Design & Discovery, 15 (11). pp. 1202-1210. ISSN 1875-628X

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Official URL: http://dx.doi.org/10.2174/157018081566618032814432...

Abstract

Background: In the current study, a series of novel thiophene chalcones (3a-g) and pyrazole containing thiophene derivatives (6a-g) were designed as potential anti-fungal agents and evaluated in silico for drug-likeness behavior. Methods: The titled compounds were synthesized using Claisen–Schmidt reaction of 3-methyl-2- thiophenecarboxaldehyde (1) with several acetophenone derivatives (2a-g) followed by cyclization reactions using hydrazine hydrate to form new compounds (6a-g) in good to excellent yield. All the synthesized compounds were characterized by IR, 1H NMR, 13C NMR and Mass spectral analysis. All the synthesized chalcones (3a-g) and pyrazole derivatives (6a-g) were screened for antifungal potency using Candida albicans (MTCC 3958) and Aspergillus niger (MTCC 9933) using fluconazole as standard drug. Results & Conclusion: The assay results revealed interesting finding that, compound 6c showed significant activity against both the tested fungal strains.

Item Type: Article
Subjects: D Physical Science > Physics
Divisions: Department of > Physics
Depositing User: manjula User
Date Deposited: 08 Nov 2019 09:54
Last Modified: 08 Nov 2019 09:54
URI: http://eprints.uni-mysore.ac.in/id/eprint/9897

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