Synthesis, characterisation and antitubercular screening of 5(4H)-oxazolone derivatives

Department of Organic Chemistry, Andhra University, Visakhapatnam-530 003, Andhra Pradesh, India

E-mail : suhasini.kl@gmail.com, murthyyln@gmail.com

Bio-Organic Chemistry Division, Indian Institute of Integrative Medicine, Jammu-180 001, J & K, India

In search of new antitubercular agents, a new series of 4-(substituted benzylidene)-2-p-tolyloxazol-5(4H)-ones (5a-h) has been designed, synthesized and subjected to evaluate their antitubercular activity for the first time against Mycobacterium tuberculosis H37Rv, in comparison with standard drugs Rifampicin and Isoniazid. The out-put of these studies disclosed that all the synthesized target molecules of the series displayed good to moderate activity with MIC values ranging 8–64 µg/mL. Compound 5e having three methoxy groups, is the most distinctive compound identified, amongst the series because of its remarkable in vitro antitubercular activity and thus may act as a promising lead molecule for further explorations.