Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl]piperidine series of histamine H3 receptor antagonists

被引：19

作者：

Berlin, M ^{[1
]}

Ting, PC ^{[1
]}

Vaccaro, WD ^{[1
]}

Aslanian, R ^{[1
]}

McCormick, KD ^{[1
]}

Lee, JF ^{[1
]}

Albanese, MM ^{[1
]}

Mutahi, MW ^{[1
]}

Piwinski, JJ ^{[1
]}

Shih, NY ^{[1
]}

Duguma, L ^{[1
]}

Solomon, DM ^{[1
]}

Zhou, W ^{[1
]}

Sher, R ^{[1
]}

Favreau, L ^{[1
]}

Bryant, M ^{[1
]}

Korfmacher, WA ^{[1
]}

Nardo, C ^{[1
]}

West, RE ^{[1
]}

Anthes, JC ^{[1
]}

Williams, SM ^{[1
]}

Wu, RL ^{[1
]}

She, HS ^{[1
]}

Rivelli, MA ^{[1
]}

Corboz, MR ^{[1
]}

Hey, JA ^{[1
]}

机构：

[1] Schering Plough Res Inst, Kenilworth, NJ 07033 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 04期

关键词：

histamine; H-3; antagonists; imidazole series; 4-[(1H-imidazol-4-y1)methyl]piperidine; decongestion; allergic rhinitis; CYP450; inhibition;

D O I：

10.1016/j.bmcl.2005.10.087

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of histamine H-3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine template displaying low CYP2D6 and CYP3A4 inhibitory profiles has been identified. Structural features responsible for the reduction of P450 activity, a typical liability of 4-substituted imidazoles, have been established. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：989 / 994

页数：6

共 11 条

[1] A new class of diamine-based human histamine H3 receptor antagonists:: 4-(aminoalkoxy)benzylamines [J].