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Medicinal Chemistry


ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

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

Author(s): Dharmarajan Sriram, Tanushree Ratan Bal and Perumal Yogeeswari

Volume 1 , Issue 3 , 2005

Page: [277 - 285] Pages: 9

DOI: 10.2174/1573406053765422

Price: $65


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 (MICs: 1.22 μg / ml).

Keywords: anti-hiv, anti-mycobacterial, anti-bacterial, isatin

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