199935-21-2Relevant articles and documents
Small molecule inhibitors of the CCR2b receptor. Part 1: Discovery and optimization of homopiperazine derivatives
Imai, Minoru,Shiota, Tatsuki,Kataoka, Ken-Ichiro,Tarby, Christine M.,Moree, Wilna J.,Tsutsumi, Takaharu,Sudo, Masaki,Ramirez-Weinhouse, Michele M.,Comer, Daniel,Sun, Chung-Ming,Yamagami, Shinsuke,Tanaka, Hiroko,Morita, Takuya,Hada, Takahiko,Greene, Jonathan,Barnum, Doug,Saunders, John,Myers, Peter L.,Kato, Yoshinori,Endo, Noriaki
, p. 5407 - 5411 (2007/10/03)
The discovery, the lead optimization, and the structure-activity relationship of N,N′-disubstituted homopiperazines are reported. N,N′-Disubstituted homopiperazine derivatives have been discovered as CC-chemokine receptor 2b (CCR2b) inhibitors with submicromolar activity in the CCR2b binding assay. A 4-substituted benzyl group on one homopiperazine nitrogen was an important moiety for binding affinity to the CCR2b receptor. The SAR for CCR2b binding affinity correlated inversely with the σ factor of the functional group on this benzyl moiety. Introduction of hydroxy groups to appropriate positions in the 3,3-diphenylpropyl group on the other homopiperazine nitrogen increased CCR2b binding activity. The synthesis of an informer library to search for alternative substructures is also described.
