1H-Pyrazole-1-carboxamidines: new inhibitors of nitric oxide synthase |
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Authors: | Younghee Lee Pavel Martsek Linda J Roman Richard B Silverman |
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Institution: | Younghee Lee, Pavel Martásek, Linda J. Roman,Richard B. Silverman, |
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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 μM. |
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