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1H-pyrazole-1-carboxamidines: new inhibitors of nitric oxide synthase
1Department of Chemistry, Northwestern University, Evanston, IL 60208-3113, USA.
Bioorganic & Medicinal Chemistry Letters
|January 2, 2001
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 Ki value of 2 microM.