Medicinal Chemistry

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

DOI: 10.2174/1573406053765422

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

Page: [277 - 285] Pages: 9

  • * (Excluding Mailing and Handling)

Abstract

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