The discovery and SAR of cyclopenta[b]furans as inhibitors of CCR2

Michael P Winters; Christopher A Teleha; Fu-An Kang; David McComsey; John C O'Neill; Cuifen Hou; Thomas Kirchner; Ping Wang; Dana Johnson; Zhihua Sui

doi:10.1016/j.bmcl.2014.03.036

The discovery and SAR of cyclopenta[b]furans as inhibitors of CCR2

Bioorg Med Chem Lett. 2014 May 1;24(9):2137-40. doi: 10.1016/j.bmcl.2014.03.036. Epub 2014 Mar 22.

Authors

Affiliations

¹ Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA. Electronic address: [email protected].
² Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.

PMID: 24685539
DOI: 10.1016/j.bmcl.2014.03.036

Abstract

The discovery of a novel series of cyclopenta[b]furans as CCR2 inhibitors is discussed. This series has excellent CCR2 potency and PK characteristics, and good cardiovascular safety.

Keywords: CCR2; Cyclopenta[b]furan; MCP-1; Thioglycolate-induced peritoneal leukocyte infiltration model; Type II diabetes.

MeSH terms

Cell Line
Chemokine CCL2 / immunology
Furans / chemistry*
Furans / pharmacology*
Humans
Receptors, CCR2 / antagonists & inhibitors*
Receptors, CCR2 / immunology

Substances

Chemokine CCL2
Furans
Receptors, CCR2