Nevirapine derivatives with broad-spectrum chemotherapeutic properties for the effective treatment of HIV/AIDS

A series of nevirapine derivatives has been synthesized in an effort to enhance the spectrum of chemotherapeutic properties for the effective treatment of AIDS and AIDS-related opportunistic infections. The nevirapine derivative bearing isoniazid moiety (3a) was found to be the most potent compound with EC50 of < 0.0636 μM, CC50 of > 1000 μM and selectivity index of > 15,723 which also exhibited 90% inhibition against Mycobacterium tuberculosis at 6.25 μg/ml. Compound 3c showed 100% inhibition against M. tuberculosis and also exhibited potent antibacterial activity against 24 pathogenic bacteria with MIC less than 1 μg/ml.