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Bipiperidinyl Carboxylic Acid Amides as Potent, Selective, and Functionally Active CCR4 Antagonists
Author(s) -
Kuhn Cyrille F.,
Bazin Marc,
Philippe Laurence,
Zhang Jiansu,
Tylaska Laurie,
Miret Juan,
Bauer Paul H.
Publication year - 2007
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2007.00551.x
Subject(s) - carboxylic acid , ccr4 , chemistry , small molecule , combinatorial chemistry , pharmacology , computational biology , chemokine , chemokine receptor , biochemistry , receptor , biology
A cell‐based assay for the chemokine G‐protein‐coupled receptor CCR4 was developed, and used to screen a small‐molecule compound collection in a multiplex format. A series of bipiperidinyl carboxylic acid amides amenable to parallel chemistry were derived that were potent and selective antagonists of CCR4. One prototype compound was shown to be active in a functional model of chemotaxis, making it a useful chemical tool to explore the role of CCR4 in asthma, allergy, diabetes, and cancer.