Synthesis, In Silico and Antifungal Studies of Novel Thiophene Analogues Containing Pyrazole Ring

Author(s): Helmi M. Al-Maqtari, Joazaizulfazli Jamalis*, Subhash Chander, Hasnah M. Sirat, Shivalingegowda Naveen, Neratur K. Lokanath, Siti P.M. Bohari, Deepak P. Bhagwat, Murugesan Sankaranarayanan

Journal Name: Letters in Drug Design & Discovery

Volume 15 , Issue 11 , 2018

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Graphical 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.

Keywords: Pyrazole, thiophene, antifungal, drug likeness, chalcone, synthesis.

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Article Details

Year: 2018
Page: [1202 - 1210]
Pages: 9
DOI: 10.2174/1570180815666180328144325
Price: $65

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