alexa Abstract | Design, Synthesis and Molecular Docking Study of substituted N-aminocarbonyl arylvinylbenzamides

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In an attempt to find a new class of antimicrobial agents, a series of novel N-aminocarbonyl arylvinyl-benzamides 5(B1-B28) were synthesized and evaluated for in vitro antifungal activity against Candida albicans (NCIM 3471), Aspergillus niger (NCIM 545), and Penicillium chrysogenum (NCIM 709). The title compounds were synthesized from nucleophilic ring opening of the appropriate arylideneoxazolones 4(A1-A3) using suitable amines. All the compounds were characterized using elemental analytical (C, H, and N) and spectral (FT-IR, 1H NMR, 13C NMR and MS) data. Among the tested compounds, N-{(1Z)-3-[(3-nitrophenyl)amino]-3-oxo-1-phenylprop-1-en-2-yl}benzamide 5(B22) was identified as a potentially excellent antifungal agent. It exhibited potent antifungal activity against Candida albicans (MIC; 2 g/mL), Aspergillus niger (MIC; 2 g/mL), and Penicillium chrysogenum (MIC; 2 g/mL) comparable with that of ketoconazole. Also compounds N-[(1Z)-3-[(2-fluorophenyl) amino]-1-( furan-2-yl)-3-oxoprop-1-en-2-yl]benzamide 5(B6) and N-{(1Z)-1-(furan-2-yl)-3-[(3-nitrophenyl) amino]-3-oxoprop-1-en-2-yl} benzamide 5(B4) also displayed good antifungal effects against all fungal strains tested. The binding mode of the tested compounds inside the sterol 14α-demethylase active site was predicted using a docking technique. Lipinski’s rule and in silico ADME pharmacokinetic parameters are within the acceptable range defined for human use thereby indicating their potential as a drug-like molecules.

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Author(s): Sanjay B. Bari, Nitin G. Haswani

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