Evaluation of a 4-aminopiperidine replacement in several series of CCR5 antagonists

Rémy C Lemoine; Ann C Petersen; Lina Setti; Lijing Chen; Jutta Wanner; Andreas Jekle; Gabrielle Heilek; André deRosier; Changhua Ji; David M Rotstein

doi:10.1016/j.bmcl.2010.02.004

Evaluation of a 4-aminopiperidine replacement in several series of CCR5 antagonists

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1830-3. doi: 10.1016/j.bmcl.2010.02.004. Epub 2010 Feb 6.

Authors

Rémy C Lemoine¹, Ann C Petersen, Lina Setti, Lijing Chen, Jutta Wanner, Andreas Jekle, Gabrielle Heilek, André deRosier, Changhua Ji, David M Rotstein

Affiliation

¹ Department of Medicinal Chemistry, Roche Palo Alto, Palo Alto, CA 94304, USA. [email protected]

PMID: 20176481
DOI: 10.1016/j.bmcl.2010.02.004

Abstract

The bicyclic 5-amino-3-azabicyclo[3.3.0]octanes were shown to be effective replacements for the conformationally restricted 4-aminopiperidine ring found in several series of CCR5 antagonists.

MeSH terms

CCR5 Receptor Antagonists*
Drug Evaluation, Preclinical*
Models, Molecular
Piperidines / chemistry*

Substances

4-aminopiperidine
CCR5 Receptor Antagonists
Piperidines