Synthetic inhibitors of cytochrome P-450 2A6: inhibitory activity, difference spectra, mechanism of inhibition, and protein cocrystallization

JK Yano, TT Denton, MA Cerny, X Zhang…

文献索引：Yano, Jason K.; Denton, Travis T.; Cerny, Matthew A.; Zhang, Xiaodong; Johnson, Eric F.; Cashman, John R. Journal of Medicinal Chemistry, 2006 , vol. 49, # 24 p. 6987 - 7001

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被引用次数: 93

摘要

A series of 3-heteroaromatic analogues of nicotine were synthesized to delineate structural and mechanistic requirements for selectively inhibiting human cytochrome P450 (CYP) 2A6. Thiophene, substituted thiophene, furan, substituted furan, acetylene, imidazole, substituted imidazole, thiazole, pyrazole, substituted pyrazole, and aliphatic and isoxazol moieties were used to replace the N-methylpyrrolidine ring of nicotine. A number of potent inhibitors ...