Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P′1 group

Philippe G. Nantermet, James C. Barrow, Stacey R. Lindsley, Marybeth Young, Shi Shan Mao, Steven Carroll, Carolyn Bailey, Michele Bosserman, Dennis Colussi, Daniel R. McMasters, Joseph P. Vacca, Harold G. Selnick

Research output: Contribution to journalArticlepeer-review

Abstract

Structural modifications of the aminopyridine P1 group of imidazole acetic acid based TAFIa inhibitors led to the discovery of the aminocyclopentyl analog 28, a 1nM TAFIa inhibitor with CLT50 functional activity of 14nM but without selectivity against CPB. While not as active, aminobutyl derivative 27 provided an improved 6.7-fold selectivity for TAFIa versus CPB.

Original languageEnglish (US)
Pages (from-to)2141-2145
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume14
Issue number9
DOIs
StatePublished - May 3 2004
Externally publishedYes

Keywords

  • Carboxypeptidase
  • Fibrinolysis
  • TAFI

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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