HIV is the most significant risk factor for many opportunistic infections like tuberculosis, hepatitis, bacterial infections etc. We designed an isatin lead compound as a novel non-nucleoside reverse transcriptase inhibitor with broad-spectrum chemotherapeutic properties for the effective treatment of AIDS and AIDS-related opportunistic infections. Compound 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-[[N4-[3′-(4′-amino-5′-trimethoxybenzyl pyrimidin-2′-yl)imino-1′-(5-chloroisatinyl)[methyl]-N1-piperazinyl]-3-quinoline carboxylic acid (14) emerged as the most potent broad-spectrum chemotherapeutic agent active against HIV, HCV, M. tuberculosis and various pathogenic bacteria.