Die Pharmazie is published by IMR Press from Volume 81 Issue 1 (2026). Previous articles were published by another publisher under the CC-BY licence, and they are hosted by IMR Press on imrpress.com as a courtesy and upon agreement.
Synthesis, anti-HIV and antitubercular activities of isatin derivatives
D. Sriram 1, P. Yogeeswari 2, K. Meena 2
Affiliations
Article Info
1 Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Pilani, 333031, India, Email: dsriram@bits-pilani.ac.in
2 Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Pilani, India
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 μg/ml), and Mycobacterium tuberculosis (MIC: 1.22 μg/ml).