کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1374215 | 981914 | 2009 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design, synthesis, and structure–activity relationship of novel CCR2 antagonists
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
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.
Discovery 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 as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 6, 15 March 2009, Pages 1830–1834
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 6, 15 March 2009, Pages 1830–1834
نویسندگان
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,