| Literature DB >> 15454235 |
Minoru Imai1, Tatsuki Shiota, Ken-ichiro Kataoka, Christine M Tarby, Wilna J Moree, Takaharu Tsutsumi, Masaki Sudo, Michele M Ramirez-Weinhouse, Daniel Comer, Chung-Ming Sun, Shinsuke Yamagami, Hiroko Tanaka, Takuya Morita, Takahiko Hada, Jonathan Greene, Doug Barnum, John Saunders, Peter L Myers, Yoshinori Kato, Noriaki Endo.
Abstract
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 sigma 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.Entities:
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Year: 2004 PMID： 15454235 DOI： 10.1016/j.bmcl.2004.08.008
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823