Aminopyrimidinimino isatin analogues: design of novel non- nucleoside HIV-1 reverse transcriptase inhibitors with broad-spectrum chemotherapeutic properties.

Abstract

PURPOSE:

HIV is the most significant risk factor for many opportunistic infections such as tuberculosis, hepatitis, bacterial infections and others. In this paper, we describe an 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.

METHODS:

The synthesis of various aminopyrimidinimino isatin derivatives was achieved in two steps and evaluated for anti-HIV, anti-HCV, antimycobacterial and antibacterial activities.

RESULTS:

Compound 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7[[N4-[3'-(4'-amino-5'-trimethoxybenzylpyrimidin-2'-yl)imino-1'-isatinyl] methyl]N1-piperazinyl]-3-quinoline carboxylic acid (14) emerged as the most potent broad-spectrum chemotherapeutic agent active against HIV, HCV, M. tuberculosis and various pathogenic bacteria. Among the synthesized compounds compound 14 and 15 emerged as more promising broad-spectrum chemotherapeutic agents.

• Authors: Dharmarajan Sriram, Tanushree Ratan Bal, Perumal Yogeeswari
• Journal: Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques (J Pharm Pharm Sci) Vol. 8 Issue 3 Pg. 565-77 (Oct 20 2005) ISSN: 1482-1826 [Electronic] Canada
• PMID: 16401403 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Aminopyridines
• Reverse Transcriptase Inhibitors
• Isatin
• HIV Reverse Transcriptase

Topics

• Aminopyridines (chemistry, pharmacology, therapeutic use)
• Animals
• Cell Line
• Drug Design
• HIV Reverse Transcriptase (antagonists & inhibitors, physiology)
• Isatin (analogs & derivatives, pharmacology, therapeutic use)
• Male
• Mice
• Reverse Transcriptase Inhibitors (chemistry, pharmacology, therapeutic use)