226249-98-5Relevant articles and documents
Small molecule antagonists of the CCR2b receptor. Part 2: Discovery process and initial structure-activity relationships of diamine derivatives
Moree, Wilna J.,Kataoka, Ken-Ichiro,Ramirez-Weinhouse, Michele M.,Shiota, Tatsuki,Imai, Minoru,Sudo, Masaki,Tsutsumi, Takaharu,Endo, Noriaki,Muroga, Yumiko,Hada, Takahiko,Tanaka, Hiroko,Morita, Takuya,Greene, Jonathan,Barnum, Doug,Saunders, John,Kato, Yoshinori,Myers, Peter L.,Tarby, Christine M.
, p. 5413 - 5416 (2007/10/03)
A lead evolution process is described that utilized the SAR of a homopiperazine series for the discovery of alternative cyclic diamine derivatives as nanomolar inhibitors of the interaction between MCP-1 and the CCR2b receptor. 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.
