Literature DB >> 18722115

Bradykinin B1 receptor antagonists: an alpha-hydroxy amide with an improved metabolism profile.

Scott D Kuduk1, Ronald K Chang, Robert M Dipardo, Christina N Di Marco, Kathy L Murphy, Richard W Ransom, Duane R Reiss, Cuyue Tang, Thomayant Prueksaritanont, Douglas J Pettibone, Mark G Bock.   

Abstract

A series of carbo- and heterocyclic alpha-hydroxy amide-derived bradykinin B1 antagonists was 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.

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Year:  2008        PMID: 18722115     DOI: 10.1016/j.bmcl.2008.07.126

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  An Efficient Boric Acid Mediated Preparation of α-Hydroxyamides.

Authors:  J Sravan Kumar; Subash C Jonnalagadda; Venkatram R Mereddy
Journal:  Tetrahedron Lett       Date:  2010-02-03       Impact factor: 2.415

Review 2.  Tetrazolium compounds: synthesis and applications in medicine.

Authors:  Cheng-Xi Wei; Ming Bian; Guo-Hua Gong
Journal:  Molecules       Date:  2015-03-27       Impact factor: 4.411

  2 in total

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