Bioorganic and Medicinal Chemistry Letters p. 5407 - 5411 (2004)
Update date:2022-09-26
Topics:
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
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.
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