期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 18, 页码 5107-5110出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.07.126
关键词
bradykinin; pain; GPCR; tetrazole
A series of carbo-and heterocyclic alpha-hydroxy amide-derived bradykinin B(1) antagonists were prepared and evaluated. A 4,4-difluorocyclohexyl alpha-hydroxy amide was incorporated along with a 2-methyl tetrazole in lieu of an oxadiazole to afford a suitable compound with good pharmacokinetic properties, CNS penetration, and clearance by multiple metabolic pathways. (C) 2008 Elsevier Ltd. All rights reserved.
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