Medicinal Chemistry

Bioisosteric Replacement and Related Analogs in the Design, Synthesis and Evaluation of Ligands for Muscarinic Acetylcholine Receptors

RR Bhandare, DJ Canney

Index: Bhandare, Richie R.; Canney, Daniel J. Medicinal Chemistry, 2014 , vol. 10, # 4 p. 361 - 375

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Abstract

Previous structure-activity relationship studies involving a series of lactone-based muscarinic ligands identified a lead compound containing a diphenylmethylpiperazine moiety (4; IC50= 340 nM). The purpose of the present work is to investigate 1, 3- benzodioxoles, 4, 4-diethyl substituted tetrahydrofurans, 5-substituted oxazolidinones and chromones as bioisosteric replacements for the lactone ring in a novel series of ...