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

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Parmee ER, He J, Mastracchio A, Edmondson SD, Colwell L, Eiermann G, Feeney WP, Habulihaz B, He H, Kilburn R, Leiting B, Lyons K, Marsilio F, Patel RA, Petrov A, Di Salvo J, Wu JK, Thornberry NA, Weber AE

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

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

PubMed ID
14684294 [ View in PubMed
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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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
VildagliptinDipeptidyl peptidase 4IC 50 (nM)34N/AN/ADetails