1H-Pyrazole-1-carboxamidines: New inhibitors of nitric oxide synthase

Younghee Lee, Pavel Martásek, Linda J. Roman, Richard B. Silverman

Research output: Contribution to journalArticle

23 Scopus citations

Abstract

1H-Pyrazole-1-carboxamidines were prepared as potential inhibitors of the three isozymes of nitric oxide synthase. All of the compounds were found to be competitive inhibitors of all three isoforms. The most selective compound prepared was 1H-pyrazole-N-(3-aminomethylanilino)-1-carboxamidine (14), which is 100-fold selective for nNOS over eNOS with a K(i) value of 2μM. (C) 2000 Elsevier Science Ltd.

Original languageEnglish (US)
Pages (from-to)2771-2774
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume10
Issue number24
DOIs
Publication statusPublished - Dec 18 2000

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ASJC Scopus subject areas

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

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