2' Biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling
2' Biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling
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DOI：
10.1016/j.bmcl.2010.04.127
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发表时间：
2010-06-15
影响因子：
2.7
通讯作者：
Jin, Jian
中科院分区：
文献类型：
--
作者：
Budzik, Brian;Garzya, Vincenzo;Jin, Jian
通过广泛探索结构-活性关系对联芳基酰胺系列的进一步优化产生了有效的和亚型选择性的M-1激动剂，例如化合物9a和9 j，其具有良好的大鼠PK性质，包括CNS渗透。介绍了这些新化合物的合成、构效关系、对M-1的亚型选择性以及DMPK性质。(C)2010爱思唯尔有限公司版权所有。
Further optimization of the biaryl amide series via extensively exploring structure-activity relationships resulted in potent and subtype selective M-1 agonists exemplified by compounds 9a and 9j with good rat PK properties including CNS penetration. Synthesis, structure-activity relationships, subtype selectivity for M-1 over M2-5, and DMPK properties of these novel compounds are described. (C) 2010 Elsevier Ltd. All rights reserved.