Discovery of N-propylurea 3-benzylpiperidines as selective CC chemokine receptor-3 (CCR3) antagonists-Science-Chemical Encyclopedia-lookchem

Discovery of N-propylurea 3-BENZYLPIPERIDINE (cas 13603-25-3)s as selective CC chemokine receptor-3 (CCR3) antagonists
Add time:08/29/2019 Source:sciencedirect.com

The discovery of novel and selective small molecule antagonists of the CC Chemokine Receptor-3 (CCR3) is presented. Simple conversion from a 4- to 3-benzylpiperidine gave improved selectivity for CCR3 over the serotonin 5HT2A receptor. Chiral resolution and exploration of mono- and disubstitution of the N-propylurea resulted in several 3-benzylpiperidine N-propylureas with CCR3 binding IC50s under 5 nM. Data from in vitro calcium mobilization and chemotaxis assays for these compounds ranged from high picomolar to low nanomolar EC50s and correlated well with antagonist binding IC50s.

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