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杂环乙酰胺和苯甲酰胺衍生物作为强效和选择性的β3-肾上腺素能受体激动剂，具有改善的啮齿动物药代动力学特征。

Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles.

机构信息

Merck Research Laboratories, Rahway, NJ 07065, USA.

出版信息

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1895-9. doi: 10.1016/j.bmcl.2010.01.130. Epub 2010 Feb 4.

DOI:10.1016/j.bmcl.2010.01.130
PMID:20181479
Abstract

A series of amide derived beta(3)-adrenergic receptor (AR) agonists is described. The discovery and optimization of several series of compounds derived from 1, is used to lay the SAR foundation for second generation beta(3)-AR agonists for the treatment of overactive bladder.

摘要

描述了一系列酰胺衍生的β3-肾上腺素能受体（AR）激动剂。发现并优化了几类源于 1 的化合物系列，为治疗膀胱过度活动症的第二代β3-AR 激动剂奠定了 SAR 基础。

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引用本文的文献

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Ther Adv Endocrinol Metab. 2011 Apr;2(2):59-64. doi: 10.1177/2042018811398517.
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Insights into the binding modes of human β₃-adrenergic receptor agonists with ligand-based and receptor-based methods.基于配体和受体方法的人β₃-肾上腺素能受体激动剂结合模式的研究。
Mol Divers. 2011 Nov;15(4):817-31. doi: 10.1007/s11030-011-9311-8. Epub 2011 Mar 20.