Discovery and synthesis of cyclohexenyl derivatives as modulators of CC chemokine receptor 2 activity

[Display omitted] A novel cyclohexenyl series of CCR2 antagonists has been discovered. This series of small, rigid compounds exhibits submicromolar binding affinity for CCR2. Modification of the substituents on the cyclohexene ring led to the identification of potent CCR2 antagonists. Progress from...

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Bibliographic Details

Published in:	Bioorganic & medicinal chemistry letters 2016-01, Vol.26 (2), p.662-666
Main Authors:	Brown, Gregory D., Shi, Qing, Delucca, George V., Batt, Douglas G., Galella, Michael A., Cvijic, Mary-Ellen, Liu, Rui-Qin, Qiu, Feng, Zhao, Qihong, Barrish, Joel C., Carter, Percy H.
Format:	Article
Language:	English
Subjects:	CCR2 CCR2 antagonist Chemokine Cyclohexenes - chemical synthesis Cyclohexenes - chemistry Cyclohexenes - pharmacology Drug Discovery GPCR Humans Models, Molecular Receptors, CCR2 - antagonists & inhibitors Receptors, CCR2 - metabolism Structure-Activity Relationship
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