降低 H3 拮抗剂 4-哌啶基脲系列中的 hERG 抑制活性。
Reduction of hERG inhibitory activity in the 4-piperidinyl urea series of H3 antagonists.
机构信息
Chemical Research, Cardiovascular/Metabolic Diseases and CNS Discovery, and Drug Metabolism and Pharmacokinetics, Merck Research Laboratories, Kenilworth, NJ 07033, USA.
出版信息
Bioorg Med Chem Lett. 2010 Apr 1;20(7):2359-64. doi: 10.1016/j.bmcl.2010.01.121. Epub 2010 Jan 28.
PMID:20188550
Abstract
Structural features of the substituted 4-piperidinyl urea analogs 1, responsible for the H3 antagonist activity, have been identified. Structure-activity relationship of the H3 receptor affinity, hERG ion channel inhibitory activity and their separation is described. Preliminary pharmacokinetic evaluation of the compounds of the series is addressed.
摘要
已确定取代的 4-哌啶基脲类似物 1 的结构特征，这些结构特征与 H3 拮抗剂活性有关。描述了 H3 受体亲和力、hERG 离子通道抑制活性及其分离的构效关系。该系列化合物的初步药代动力学评价也已进行。
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