Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012

通过对 MLPCN 探针 ML012 的持续优化，开发出选择性更高的 M(1) 拮抗剂

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作者：Melancon,Bruce J,Lamers,Alexander P,Bridges,Thomas M,Sulikowski,Gary A,Utley,Thomas J,Sheffler,Douglas J,Noetzel,Meredith J,Morrison,Ryan D,Daniels,J Scott,Niswender,Colleen M,Jones,Carrie K,Conn,P Jeffrey,Lindsley,Craig W,Wood,Michael R
期刊：Bioorganic & Medicinal Chemistry Letters影响因子：2.200
时间：2012起止号：2012 Jan 15;22(2):1044-8
doi：10.1016/j.bmcl.2011.11.110

Abstract

This Letter describes the continued optimization of an MLPCN probe molecule (ML012) through an iterative parallel synthesis approach. After exploring extensive modifications throughout the parent structure, we arrived at a more highly M(1)-selective antagonist, compound 13l (VU0415248). Muscarinic subtype selectivity across all five human and rat receptors for 13l, along with rat selectivity for the lead compound (ML012), is presented.

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