TY - JOUR
T1 - 1H-Pyrazole-1-carboxamidines
T2 - New inhibitors of nitric oxide synthase
AU - Lee, Younghee
AU - Martásek, Pavel
AU - Roman, Linda J.
AU - Silverman, Richard B.
N1 - Funding Information:
We are grateful to the National Institutes of Health for financial support of this research to R.B.S. (GM49725) and Bettie Sue Siler Masters (GM52419) and to the Robert A. Welch Foundation (AQ-1192) for financial support to B.S.S.M, in whose lab P.M. and L.J.R. work. Sincere thanks go to Professor Michael A. Marletta (University of Michigan) for the E. coli cells which express murine macrophage iNOS.
PY - 2000/12/18
Y1 - 2000/12/18
N2 - 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.
AB - 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.
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U2 - 10.1016/S0960-894X(00)00573-4
DO - 10.1016/S0960-894X(00)00573-4
M3 - Article
C2 - 11133088
AN - SCOPUS:0034684773
SN - 0960-894X
VL - 10
SP - 2771
EP - 2774
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 24
ER -