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Small molecule antagonists for chemokine CCR3 receptors by Lianne I. Willems; Ad P. IJzerman is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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## Abstract The chemokine receptor CCR3 is believed to play a role in the development of allergic diseases such as asthma, atopic dermatitis, and allergic rhinitis. Despite the conflicting results that have been reported regarding the importance of eosinophils and CCR3 in allergic inflammation, inhibition of this receptor with small molecule antagonists is thought to provide a valuable approach for the treatment of these diseases. This review describes the structure–activity relationships (SAR) of small molecule CCR3 antagonists as reported in the scientific and patent literature. Various chemical classes of small molecule CCR3 antagonists have been described so far, including (bi)piperidine and piperazine derivatives, __N__‐arylalkylpiperidine urea derivatives and (__N__‐ureidoalkyl)benzylpiperidines, phenylalanine derivatives, morpholinyl derivatives, pyrrolidinohydroquinazolines, arylsulfonamides, amino‐alkyl amides, imidazole‐ and pyrimidine‐based antagonists, and bicyclic diamines. The (__N__‐ureidoalkyl)benzylpiperidines are the best studied class in view of their generally high affinity and antagonizing potential. For many of these antagonists subnanomolar IC~50~ values were

Who reads Small molecule antagonists for chemokine CCR3 receptors?

Author

Lianne I. Willems; Ad P. IJzerman

Publisher

John Wiley and Sons; Wiley (John Wiley & Sons); John Wiley & Sons Inc.; Wiley (ISSN 0198-6325)

Published

2010

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)