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Bioorg Med Chem Lett. 2004 Jan 5;14(1):43-6.

4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.

Author information

1
Department of Medicinal Chemistry, Merck & Co. Inc., PO Box 2000, Rahway, NJ 07065, USA. emma_parmee@merck.com

Abstract

Substituted 4-amino cyclohexylglycine analogues were evaluated for DP-IV inhibitory properties. Bis-sulfonamide 15e was an extremely potent 2.6 nM inhibitor of the enzyme with excellent selectivity over all counterscreens. 2,4-difluorobenzenesulfonamide 15b and 1-naphthyl amide 16b, however, combined an acceptable in vitro profile with good pharmacokinetic properties in the rat, and 15b was orally efficacious at 3 mpk in an OGTT in lean mice.

PMID:
14684294
DOI:
10.1016/j.bmcl.2003.10.016
[Indexed for MEDLINE]

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