期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 4, 页码 1374-1377出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.01.016
关键词
CCR2; chemokine; antagonist
In an effort to shed light on the active binding conformation of our 3-amino-1-alkyl-cyclopentane carboxamide CCR2 antagonists, we prepared several conformationally constrained analogs resulting from backbone cyclization. Evaluation of CCR2 binding affinities for these analogs gave insight into the optimal relative positions of the piperidine and benzylamide moieties while simultaneously leading to the discovery of a new, potent lead type based upon a spirocyclic acetal scaffold. (c) 2008 Elsevier Ltd. All rights reserved.
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