Synthesis of 2-methyl-4-quinolone-3-acetic acids with potential antibacterial activity

Abstract

A number of quinolone-3-acetic acids were synthesized by cyclocondensation of substituted anilines with diethyl acetylsuccinate in the presence of phosphorous pentoxide and followed by base hydrolysis of the resultant esters to form respective acids. All synthesized compounds were found to exhibit antibacterial activities against a range of gram-positive (Bacillus subtilis, Staphylococcus aureus) and gram-negative bacteria (Shigella sonnei, Escherichia coli, Pseudomonas aeruginosa and Salmonella typhi) by broth dilution method. All the compounds exhibited antibacterial activities comparable to fluoroquinolones and in some cases even better activity was found. These findings suggest a great potential of these compounds for screening and use as antibacterial compounds for further studies with a battery of bacteria.