Synthesis and Microbiological Evaluation of Substituted 1,3-Oxazol-5(4H)-One Derivatives

The major drawback of current treatment of infectious diseases are challenging due to resistance to antimicrobial agents and their side effects. 1,3-oxazol-5(4H)-one(oxazolinone) derivatives are the heterocyclic compounds with considerable therapeutic and biological properties. In this view, the series of 4-((5-oxo-2-phenyloxazol-4(5H)-ylidene)-methyl)-phenyl benzoatederivatives with different substitution were synthesized and evaluated for antimicrobial activity. 4-((5-oxo-2-phenyloxazol-4(5H)-ylidene)methyl)-phenyl benzoatederivatives was synthesized by first SchottenBaumann reaction get the benzoylglycine derivatives and then after the Erlenmeyer Plochlazlactone reaction produced azlactone derivatives which on reaction with substituted benzoyl chloride produced final compounds.

In antibacterial activity and antifungal activity, compounds IVe and IVf showed highest activity and IVc shown lowest against S. aureus, B. subtilis and C. albicans. While compounds IVh showed highest activity against E. coli. Among all the synthesized compounds, compounds with p-chloro phenyl group at second position of oxazolinone ring are found to be more active compared to the p-methoxy phenyl and unsubstituted phenyl group at second position of oxazalinone.