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.
Graphical Abstract
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