| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374215 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
A series of novel 1-aminocyclopentyl-3-carboxyamides incorporating substituted tetrahydropyran moieties have been synthesized and subsequently evaluated for their antagonistic activity against the human CCR2 receptor. Among them analog 59 was found to posses potent antagonistic activity.
Graphical abstractDiscovery of a novel series of 3-aminocyclopentanecarboxamide CCR2 receptor antagonists are presented herein. These compounds demonstrate high affinity and functional inhibition of hCCR2 receptors. A discussion on SAR along with the cross species PK profile for the best analog (59) is also included.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Shankaran Kothandaraman, Karla L. Donnely, Gabor Butora, Richard Jiao, Alexander Pasternak, Gregori J. Morriello, Stephen D. Goble, Changyou Zhou, Sander G. Mills, Malcolm MacCoss, Pasquale P. Vicario, Julia M. Ayala, Julie A. DeMartino, Mary Struthers,