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 Citations (Scopus)

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
StatePublished - Dec 18 2000

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Nitric Oxide Synthase
Isoenzymes
Protein Isoforms
pyrazole
pyrazole-1-carboxamidine

ASJC Scopus subject areas

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

Cite this

Lee, Y., Martásek, P., Roman, L. J., & Silverman, R. B. (2000). 1H-Pyrazole-1-carboxamidines: New inhibitors of nitric oxide synthase. Bioorganic and Medicinal Chemistry Letters, 10(24), 2771-2774.

1H-Pyrazole-1-carboxamidines : New inhibitors of nitric oxide synthase. / Lee, Younghee; Martásek, Pavel; Roman, Linda J.; Silverman, Richard B.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 10, No. 24, 18.12.2000, p. 2771-2774.

Research output: Contribution to journalArticle

Lee, Y, Martásek, P, Roman, LJ & Silverman, RB 2000, '1H-Pyrazole-1-carboxamidines: New inhibitors of nitric oxide synthase', Bioorganic and Medicinal Chemistry Letters, vol. 10, no. 24, pp. 2771-2774.
Lee Y, Martásek P, Roman LJ, Silverman RB. 1H-Pyrazole-1-carboxamidines: New inhibitors of nitric oxide synthase. Bioorganic and Medicinal Chemistry Letters. 2000 Dec 18;10(24):2771-2774.
Lee, Younghee ; Martásek, Pavel ; Roman, Linda J. ; Silverman, Richard B. / 1H-Pyrazole-1-carboxamidines : New inhibitors of nitric oxide synthase. In: Bioorganic and Medicinal Chemistry Letters. 2000 ; Vol. 10, No. 24. pp. 2771-2774.
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