Author/Authors :
Park، نويسنده , , Woul Seong and Jun، نويسنده , , Mi Ae and Shin، نويسنده , , Mi Sik and Kwon، نويسنده , , Sung Wook and Kang، نويسنده , , Seung Kyu and Kim، نويسنده , , Ki Young and Dal Rhee، نويسنده , , Sang and Bae، نويسنده , , Myung Ae and Narsaiah، نويسنده , , Banda and Lee، نويسنده , , Duck Hyung and Cheon، نويسنده , , Hyae Gyeong and Ahn، نويسنده , , Jin Hee and Kim، نويسنده , , Sung Soo، نويسنده ,
Abstract :
A series of triazepane derivatives such as (R)-3-amino-1-(1,2,5-triazepan-1-yl)-4-(2,4,5-trifluorophenyl)butan-1-ones (7, 13a–p) and (R)-3-amino-1-(1,2,5-triazepan-5-yl)-4-(2,4,5-trifluorophenyl)butan-1-ones (17a–e) was synthesized and evaluated for their ability to inhibit dipeptidyl peptidase IV (DPP-IV) enzyme. Compounds with the acid moiety were found to be potent inhibitors of DPP-IV without inhibiting CYP 3A4. Among them, compound 13p ((R)-4-[1-acetyl-2-{3-amino-4-(2,4,5-trifluorophenyl)butanoyl-1,2,5-triazepan-5-carbonyl}benzoic acid]) showed a good in vitro activity without inhibiting CYP.
Keywords :
Dipeptidyl peptidase IV , incretin , diabetes , Triazepane
