Aminopyrimidinimino Isatin Analogues: Design and Synthesis of Novel Non- Nucleoside HIV-1 Reverse Transcriptase Inhibitors with Broad- Spectrum Anti-Microbial Properties

HIV is the most significant risk factor for many opportunistic infections like tuberculosis, bacterial infections etc. In this paper, we designed aminopyrimidinimino 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-ethyl-6-fluoro-1,4-dihydro-4-oxo-7[[N4-[3'-(4'-amino-5'-chloroben-zylpyrimidin- 2'-yl)imino-1'-(5-methylisatinyl)] methyl]N1-piperazinyl]-3-quinoline carboxylic acid (10) emerged as the most potent broad-spectrum chemotherapeutic agent active against HIV-1 replication (EC50: 9.4 μg / ml), M. tuberculosis (MIC: 3.13 μg / ml) and various pathogenic bacteria (MIC's: 1.22 μg / ml).