Small molecule antagonists of the CCR2b receptor. Part 2: Discovery process and initial structure-activity relationships of diamine derivatives

  • Bioorg Med Chem Lett. 2004 Nov 1;14(21):5413-6. doi: 10.1016/j.bmcl.2004.08.009.
Wilna J Moree  1 ,  Ken-ichiro Kataoka ,  Michele M Ramirez-Weinhouse ,  Tatsuki Shiota ,  Minoru Imai ,  Masaki Sudo ,  Takaharu Tsutsumi ,  Noriaki Endo ,  Yumiko Muroga ,  Takahiko Hada ,  Hiroko Tanaka ,  Takuya Morita ,  Jonathan Greene ,  Doug Barnum ,  John Saunders ,  Yoshinori Kato ,  Peter L Myers ,  Christine M Tarby
Affiliations
  • 1. Deltagen Research Laboratories, 4570 Executive Drive, Suite 400, San Diego, CA 92121, USA. [email protected]
PMID: 15454236 DOI: 10.1016/j.bmcl.2004.08.009
Abstract

Structure-activity relationships (SAR) of a weakly active class of CCR2b inhibitors were utilized to initiate a lead evolution program employing the Drug Discovery Engine. Several alternative structural series have been discovered that display nanomolar activity in the CCR2b binding and CCR2b-mediated chemotaxis assays.