Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas - The effect of capping the distal basic piperidine nitrogen
Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas - The effect of capping the distal basic piperidine nitrogen
复制标题
DOI：
10.1016/j.bmcl.2008.09.032
复制
发表时间：
2008-10-15
影响因子：
2.7
通讯作者：
Lindsley, Craig W.
中科院分区：
文献类型：
--
作者：
Miller, Nicole R.;Daniels, R. Nathan;Lindsley, Craig W.
这封信描述了进一步的合成和SAR，开发通过迭代的类似物库的方法，类似物的高度选择性的M1变构激动剂TBPB通过删除远端碱性哌啶氮形成酰胺，磺酰胺和脲。尽管碱性和拓扑结构发生了很大变化，但M1的选择性仍得以保持。(C)2008爱思唯尔有限公司保留所有权利。
This letter describes the further synthesis and SAR, developed through an iterative analog library approach, of analogs of the highly selective M1 allosteric agonist TBPB by deletion of the distal basic piperidine nitrogen by the formation of amides, sulfonamides and ureas. Despite the large change in basicity and topology, M1 selectivity was maintained. (C) 2008 Elsevier Ltd. All rights reserved.