Al-Maqtari, Helmi M. and Jamalis, Joazaizulfazli and Chander, Subhash and M. Sirat, Hasnah and Naveen, Shivalingegowda and Lokanath, Neratur K. and M. Bohari, Siti P. and Bhagwat, Deepak P. and Sankaranarayanan, Murugesan (2018) Synthesis, in silico and antifungal studies of novel thiophene analogues containing pyrazole ring. Letters in Drug Design and Discovery, 15 (11). pp. 1202-1210. ISSN 1570-1808
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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 |
|---|---|
| Uncontrolled Keywords: | antifungal, chalcone, drug likeness, pyrazole, synthesis, thiophene |
| Subjects: | Q Science > QD Chemistry |
| Divisions: | Science |
| ID Code: | 85669 |
| Deposited By: | Yanti Mohd Shah |
| Deposited On: | 20 Jul 2020 01:24 |
| Last Modified: | 20 Jul 2020 01:24 |
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