Document Report Card

Basic Information

ID: ALA1156303

Journal: Bioorg Med Chem Lett

Title: Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists.

Authors: Miller NR, Daniels RN, Lee D, Conn PJ, Lindsley CW.

Abstract: This Letter describes the synthesis and SAR, developed through an iterative analog library approach, of a novel series of selective M(1) mAChR 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 M(1) antagonist IC(50)s in the 350 nM to >10 microM range with varying degrees of functional selectivity versus M(2)-M(5).

CiteXplore: 20202841

DOI: 10.1016/j.bmcl.2010.02.041