Abstract
Background: Condensation of 3-acetyl coumarin (1) with 2‐(4-methoxy- benzylidene) malononitrile (2) in ammonium acetate/acetic acid or absolute ethanol/piperidine affords pyridine (3) and chromen-2-one (4) derivatives, respectively. Methods: In this study, the reaction of 3 with an electrophilic reagent, namely, formic acid, acetic anhydride and formamide afforded the pyridopyrimidinone and pyridine derivatives (6- 9). Also, treatment of 3 with different aromatic aldehydes, carbon disulfide, NaN3/NH4Cl, 2- (4-methoxybenzylidene)malononitrile and acetophenone afforded pyridopyrimidinone, carbamodithioic acid, tetrazol-5-yl-chromen-2-one, 2H-chromen-2-one, and pyridine derivatives (10-14), respectively. Results: This study synthesized coumarins with antimicrobial activity and verified the structure and purity of the synthesized compounds using spectral data. Conclusion: The new compounds were evaluated in vitro for their antimicrobial activity against gram-positive bacteria (Staphylococcus aureus, Methicillin-resistant Staphylococcus aureus) and gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa), in addition to fungus (Candida albicans). The investigated substances 3 and 14 presented good activity against MRSA, E. coli, P. aeruginosa and C. albicans, while compounds 9, 10a-c, 11, 12 and 13 exhibited good to moderate activity.
Published Version
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