199935-06-3Relevant academic research and scientific papers
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.
DIARYLALKYL CYCLIC DIAMINE DERIVATIVES AS CHEMOKINE RECEPTOR ANTAGONISTS
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, (2008/06/13)
Cyclic diamines of formula (I) or their pharmacologically acceptable acid addition salts, and their medical applications are described. These compounds inhibit the action of chemokines such as MIP-la and/or MCP-l on target cells, and are useful as a therapeutic drug and/or preventative drug in diseases, such as atherosclerosis, rheumatoid arthritis, and the like where blood monocytes and lymphocytes infiltrate into tissues.
