PMID: 16649536May 3, 2006Paper

Synthesis, anti-HIV and antitubercular activities of isatin derivatives

Die Pharmazie
Dharmarajan SriramK Meena

Abstract

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 microg/ml), and Mycobacterium tuberculosis (MIC: 1.22 microg/ml).

Citations

Jan 1, 2010·Acta Crystallographica. Section E, Structure Reports Online·Hoong-Kun FunYan Zhang
Nov 15, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Pavol TisovskýAnton Gáplovský
Sep 26, 2020·Current Organic Synthesis·Garima ChauhanShaik Khasimbi

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