Title of article :
From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part II: Acyclic replacements for the (3S)-3-benzylpiperidine in a series of potent CCR3 antagonists
Author/Authors :
Daniel S. Gardner، نويسنده , , Joseph B. Santella III، نويسنده , , Andrew J. Tebben، نويسنده , , Douglas G. Batt، نويسنده , , Soo S. Ko، نويسنده , , Sarah C. Traeger، نويسنده , , Patricia K. Welch، نويسنده , , Eric A. Wadman، نويسنده , , Paul Davies، نويسنده , , Percy H. Carter، نويسنده , , John V. Duncia، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2008
Abstract :
Conformational analysis of the 3-benzylpiperidine in CCR3 antagonist clinical candidate 1 (BMS-639623) predicts that the benzylpiperidine may be replaced by acyclic, conformationally stabilized, anti-1,2-disubstituted phenethyl- and phenpropylamines. Ab initio calculations, enantioselective syntheses, and evaluation in CCR3 binding and chemotaxis assays of anti-1-methyl-2-hydroxyphenethyl- and phenpropylamine-containing CCR3 antagonists support this conformational correlation.
Keywords :
asthma , 3-Benzylpiperidine , CCR3 antagonist , Eosinophil chemotaxis , Acyclic scaffold , Conformational analysis , Ab initio
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
