Synthesis, SAR and evaluation of [1,4']-bipiperidinyl-4-yl-imidazolidin-2-one derivatives as novel CCR5 antagonists

David M Rotstein; Stephen D Gabriel; Nicole Manser; Lubov Filonova; Fernando Padilla; Surya Sankuratri; Changhua Ji; Andre deRosier; Marianna Dioszegi; Gabrielle Heilek; Andreas Jekle; Paul Weller; Pamela Berry

doi:10.1016/j.bmcl.2010.04.077

Synthesis, SAR and evaluation of [1,4']-bipiperidinyl-4-yl-imidazolidin-2-one derivatives as novel CCR5 antagonists

Bioorg Med Chem Lett. 2010 Jun 1;20(11):3219-22. doi: 10.1016/j.bmcl.2010.04.077. Epub 2010 Apr 22.

Authors

David M Rotstein¹, Stephen D Gabriel, Nicole Manser, Lubov Filonova, Fernando Padilla, Surya Sankuratri, Changhua Ji, Andre deRosier, Marianna Dioszegi, Gabrielle Heilek, Andreas Jekle, Paul Weller, Pamela Berry

Affiliation

¹ Roche Palo Alto LLC, 3431 Hillview Avenue, Palo Alto, CA 94304, USA. [email protected]

PMID: 20457517
DOI: 10.1016/j.bmcl.2010.04.077

Abstract

Elaboration of our previously disclosed spiropiperidine template led to the development of a series of novel CCR5 antagonists. Results of SAR exploration and preliminary lead characterization are described.

MeSH terms

Animals
CCR5 Receptor Antagonists*
Cell Line
Drug Evaluation, Preclinical
Humans
Imidazolidines / chemical synthesis*
Imidazolidines / chemistry
Imidazolidines / pharmacokinetics
Imidazolidines / pharmacology*
Rats
Structure-Activity Relationship

Substances

CCR5 Receptor Antagonists
Imidazolidines