Synthesis and optimization of novel and selective muscarinic M(3) receptor antagonists

Naresh Kumar; Kirandeep Kaur; Shelly Aeron; Sankaranarayanan Dharmarajan; Arun D V Silamkoti; Anita Mehta; Suman Gupta; Anita Chugh; Jang B Gupta; Mohammad Salman; Venkata P Palle; Ian A Cliffe

doi:10.1016/j.bmcl.2007.06.081

Synthesis and optimization of novel and selective muscarinic M(3) receptor antagonists

Bioorg Med Chem Lett. 2007 Sep 15;17(18):5256-60. doi: 10.1016/j.bmcl.2007.06.081. Epub 2007 Jun 30.

Authors

Naresh Kumar¹, Kirandeep Kaur, Shelly Aeron, Sankaranarayanan Dharmarajan, Arun D V Silamkoti, Anita Mehta, Suman Gupta, Anita Chugh, Jang B Gupta, Mohammad Salman, Venkata P Palle, Ian A Cliffe

Affiliation

¹ Ranbaxy Research Laboratories, New Drug Discovery Research, Department of Medicinal Chemistry, Gurgaon, Haryana 122 001, India. [email protected]

PMID: 17629699
DOI: 10.1016/j.bmcl.2007.06.081

Abstract

A series of constrained piperidine analogues were synthesized as novel muscarinic M(3) receptor antagonists. Evaluation of these compounds in binding assays revealed that they not only have high affinity for the M(3) receptor but also have high selectivity over the M(2) receptor.

MeSH terms

Muscarinic Antagonists / chemical synthesis*
Muscarinic Antagonists / chemistry
Muscarinic Antagonists / pharmacology*
Receptor, Muscarinic M3 / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Muscarinic Antagonists
Receptor, Muscarinic M3