Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists.
Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists.
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作为毒蕈碱乙酰胆碱受体亚型 1 (M1) 拮抗剂的 N-(4-(4-烷基哌嗪-1-基)苯基)苯甲酰胺的合成和 SAR。
DOI：
10.1016/j.bmcl.2010.02.041
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发表时间：
2010
影响因子：
2.7
通讯作者：
Lindsley,CraigW
中科院分区：
文献类型：
--
作者：
Miller,NicoleR;Daniels,RNathan;Lee,David;Conn,PJeffrey;Lindsley,CraigW
This Letter describes the synthesis and SAR, developed through an iterative analog library approach, of a novel series of selective M1mAChR antagonists, based on an N-(4-(4-alkylpiperazin-1-yl)phenyl)benzamide scaffold for the potential treatment of Parkinson’s disease, dystonia and other movement disorders. Compounds in this series possess M1antagonist IC50s in the 350nM to >10μM range with varying degrees of functional selectivity versus M2–M5.
