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Bioorg Med Chem Lett ; 20(7): 2099-102, 2010 Apr 01.
Article in English | MEDLINE | ID: mdl-20223662

ABSTRACT

Novel 3-aminopyrrolidine derivatives were synthesized and evaluated for their antagonistic activity against human chemokine receptor 2. Structure-activity studies on 3-aminopyrrolidine incorporating heteroatomic carbocycle moieties led to piperidine compound 19, and piperazine compounds 42, 47 and 49 as highly potent hCCR2 antagonists.


Subject(s)
Pyrrolidines/chemistry , Pyrrolidines/pharmacology , Receptors, CCR2/antagonists & inhibitors , Receptors, CCR2/metabolism , Cell Line , Chemotaxis/drug effects , Humans , Inhibitory Concentration 50 , Protein Binding/drug effects , Pyrrolidines/chemical synthesis , Structure-Activity Relationship
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