Title of article
Discovery of N-propylurea 3-benzylpiperidines as selective CC chemokine receptor-3 (CCR3) antagonists
Author/Authors
Jeffrey G. Varnes، نويسنده , , Daniel S. Gardner، نويسنده , , Joseph B. Santella III، نويسنده , , John V. Duncia، نويسنده , , Melissa Estrella، نويسنده , , Paul S Watson، نويسنده , , Cheryl M Clark، نويسنده , , Soo S. Ko، نويسنده , , Patricia Welch، نويسنده , , Maryanne Covington، نويسنده , , Nicole Stowell، نويسنده , , Eric Wadman، نويسنده , , Paul Davies، نويسنده , , Kimberley Solomon، نويسنده , , Robert C Newton، نويسنده , , George L. Trainor، نويسنده , , Carl P. Decicco، نويسنده , , Dean A. Wacker، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
5
From page
1645
To page
1649
Abstract
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794252
Link To Document