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

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[[N(4)-[3'-(4'-amino-5'-chloroben-zylpyrimidin-2'-yl)imino-1'-(5-methylisatinyl)] methyl]N(1)-piperazinyl]-3-quinoline carboxylic acid (10) emerged as the most potent broad-spectrum chemotherapeutic agent active against HIV-1 replication (EC(50): 9.4 microg /ml), M. tuberculosis (MIC: 3.13 microg /ml) and various pathogenic bacteria (MIC's: 1.22 microg /ml).
AuthorsDharmarajan Sriram, Tanushree Ratan Bal, Perumal Yogeeswari
JournalMedicinal chemistry (Shariqah (United Arab Emirates)) (Med Chem) Vol. 1 Issue 3 Pg. 277-85 (May 2005) ISSN: 1573-4064 [Print] Netherlands
PMID16787323 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)
Chemical References
  • 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-((N4-(3'-(4'-amino-5'-chlorobenzylpyrimidin-2'-yl)imino-1'-(5-methylisatinyl))methyl)-N1-piperazinyl)-3-quinolinecarboxylic acid
  • Anti-Infective Agents
  • Imines
  • Indoles
  • Pyrimidines
  • Quinolines
  • Reverse Transcriptase Inhibitors
  • Lead
  • Isatin
  • HIV Reverse Transcriptase
Topics
  • Anti-Infective Agents (chemical synthesis, chemistry, pharmacology)
  • Bacteria (drug effects)
  • Cells, Cultured
  • Drug Design
  • HIV Reverse Transcriptase (antagonists & inhibitors)
  • HIV-1 (drug effects, enzymology)
  • Humans
  • Imines (chemistry)
  • Indoles (chemical synthesis, chemistry, pharmacology)
  • Isatin (chemistry)
  • Lead (chemistry)
  • Mycobacterium tuberculosis (drug effects)
  • Pyrimidines (chemistry)
  • Quinolines (chemical synthesis, chemistry, pharmacology)
  • Reverse Transcriptase Inhibitors (chemical synthesis, chemistry, pharmacology)
  • Virus Replication (drug effects)

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