Title of article
Dihydropyridine neuropeptide Y Y1 receptor antagonists 2: bioisosteric urea replacements Original Research Article
Author/Authors
Graham S. Poindexter، نويسنده , , Marc A. Bruce، نويسنده , , J. Guy Breitenbucher، نويسنده , , Mendi A. Higgins، نويسنده , , S.-Y Sit، نويسنده , , Jeffrey L. Romine، نويسنده , , Scott W Martin، نويسنده , , Sally P Ward، نويسنده , , Rachel T. McGovern، نويسنده , , Wendy Clarke، نويسنده , , John Russell، نويسنده , , Ildiko Antal-Zimanyi، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
15
From page
507
To page
521
Abstract
Structure–activity studies around the urea linkage in BMS-193885 (4a) identified the cyanoguanidine moiety as an effective urea replacement in a series of dihydropyridine NPY Y1 receptor antagonists. In comparison to urea 4a (Ki=3.3 nM), cyanoguanidine 20 (BMS-205749) displayed similar binding potency at the Y1 receptor (Ki=5.1 nM) and full functional antagonism (Kb=2.6 nM) in SK-N-MC cells. Cyanoguanidine 20 also demonstrated improved permeability properties in Caco-2 cells in comparison to urea 4a (43 vs 19 nm/s).
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2004
Journal title
Bioorganic and Medicinal Chemistry
Record number
1302884
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