Synthesis, anti-HIV and antitubercular activities of isatin derivatives
HIV is the most significant risk factor for many opportunistic infections like tuberculosis. In this study, we designed an isatinimino lead compound as a novel non-nucleoside reverse transcriptase inhibitor with antimycobacterial properties for the effective treatment of AIDS and AIDS-related tuberculosis. Among the compounds sythesized, 1-cyclopropyl-6-fluoro-8-methoxy-1,4-dihydro-4- oxo-7[[N4-[3′-[(4,6-dimethylpyrimidin-2-yl)benzenesulfonamido- 4-yl]imino-1′-(5-fluoroisatinyl)]methyl]-3-methyl N1- piperazinyl]-3-quinoline carboxylic acid (9) emerged as the most potent broad-spectrum chemotherapeutic agent active against HIV (EC50: 12.1 μg/ml), and Mycobacterium tuberculosis (MIC: 1.22 μg/ml).
Sriram,Yogeeswari,Meena
p. 274 - 277
(2007/10/03)
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