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新型选择性毒蕈碱M(3)受体拮抗剂的合成与优化

Synthesis and optimization of novel and selective muscarinic M(3) receptor antagonists.

作者信息

Kumar Naresh, Kaur Kirandeep, Aeron Shelly, Dharmarajan Sankaranarayanan, Silamkoti Arun D V, Mehta Anita, Gupta Suman, Chugh Anita, Gupta Jang B, Salman Mohammad, Palle Venkata P, Cliffe Ian A

机构信息

Ranbaxy Research Laboratories, New Drug Discovery Research, Department of Medicinal Chemistry, Gurgaon, Haryana 122 001, India.

出版信息

Bioorg Med Chem Lett. 2007 Sep 15;17(18):5256-60. doi: 10.1016/j.bmcl.2007.06.081. Epub 2007 Jun 30.

Abstract

A series of constrained piperidine analogues were synthesized as novel muscarinic M(3) receptor antagonists. Evaluation of these compounds in binding assays revealed that they not only have high affinity for the M(3) receptor but also have high selectivity over the M(2) receptor.

摘要

合成了一系列受约束的哌啶类似物作为新型毒蕈碱M(3)受体拮抗剂。在结合试验中对这些化合物进行评估发现,它们不仅对M(3)受体具有高亲和力,而且对M(2)受体具有高选择性。

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