Title of article
Bradykinin B1 receptor antagonists: An α-hydroxy amide with an improved metabolism profile
Author/Authors
Scott D. Kuduk، نويسنده , , Ronald K. Chang، نويسنده , , Robert M. DiPardo، نويسنده , , Christina N. Di Marco، نويسنده , , Kathy L. Murphy، نويسنده , , Richard W. Ransom، نويسنده , , Duane R. Reiss، نويسنده , , Cuyue Tang، نويسنده , , Thomayant Prueksaritanont، نويسنده , , Douglas J. Pettibone، نويسنده , , Mark G. Bock، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
4
From page
5107
To page
5110
Abstract
A series of carbo- and heterocyclic α-hydroxy amide-derived bradykinin B1 antagonists was prepared and evaluated. A 4,4-difluorocyclohexyl α-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.
Keywords
pain , tetrazole , GPCR , bradykinin
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799959
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