期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 50, 期 21, 页码 5161-5167出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm051292n
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The B1 receptor is an attractive target for the treatment of pain and inflammation. A series of 3-carboxamido5-phenacylamino pyrazole B1 receptor antagonists are described that exhibit good potency against B1 and high selectivity over B2. Initially, N-unsubstituted pyrazoles were studied, but these compounds suffered from extensive glucuronidation in primates. This difficulty could be surmounted by the use of N-substituted pyrazoles. Optimization efforts culminated in compound 41, which has high receptor potency and metabolic stability.
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