Synthesis and structure-activity relationships of 2-(1,4′-bipiperidin-1′-yl)thiazolopyridine as H3 receptor antagonists
Synthesis and structure-activity relationships of 2-(1,4′-bipiperidin-1′-yl)thiazolopyridine as H3 receptor antagonists
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DOI：
10.1016/j.bmcl.2009.09.006
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发表时间：
2009-11-01
影响因子：
2.7
通讯作者：
Lachowicz, Jean
中科院分区：
文献类型：
--
作者：
Rao, Ashwin U.;Palani, Anandan;Lachowicz, Jean
合成了一系列2-（1，4 ′-联哌啶-1 ′-基）噻唑并吡啶类化合物，并对其作为非咪唑类组胺H-3受体拮抗剂进行了评价。在吡啶环的6位引入多样性旨在增强体外效力并降低hERG活性。这些新的噻唑并吡啶拮抗剂的构效关系进行了讨论。(c)2009爱思唯尔有限公司保留所有权利。
A series of 2-(1,4'-bipiperidine-1'-yl)thiazolopyridines was synthesized and evaluated as a new lead of non-imidazole histamine H-3 receptor antagonists. Introduction of diversity at the 6-position of the pyridine ring was designed to enhance in vitro potency and decrease hERG activity. The structure-activity relationships for these new thiazolopyridine antagonists are discussed. (c) 2009 Elsevier Ltd. All rights reserved.