Title of article :
(3R)-3-Amino-4-(2,4,5-trifluorophenyl)-N-{4-[6-(2-methoxyethoxy)benzothiazol-2-yl]tetrahydropyran-4-yl}butanamide as a potent dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
Author/Authors :
Aiko Nitta، نويسنده , , Hideaki Fujii، نويسنده , , Satoshi Sakami، نويسنده , , Yutaka Nishimura، نويسنده , , Tomofumi Ohyama، نويسنده , , Mikiya Satoh، نويسنده , , Junko Nakaki، نويسنده , , Shiho Satoh، نويسنده , , Chifumi Inada، نويسنده , , Hideki Kozono، نويسنده , , Hiroki Kumagai، نويسنده , , Masahiro Shimamura، نويسنده , , Tominaga Fukazawa، نويسنده , , Hideki Kawai، نويسنده ,
Abstract :
Novel series of 3-amino-N-(4-aryl-1,1-dioxothian-4-yl)butanamides and 3-amino-N-(4-aryltetrahydropyran-4-yl)butanamides were synthesized and evaluated as dipeptidyl peptidase IV (DPP-IV) inhibitors. Derivatives incorporating the 6-substituted benzothiazole group showed highly potent DPP-IV inhibitory activity. Oral administration of (3R)-3-amino-4-(2,4,5-trifluorophenyl)-N-{4-[6-(2-methoxyethoxy)benzothiazol-2-yl]tetrahydropyran-4-yl}butanamide (12u) reduced blood glucose excursion in an oral glucose tolerance test.
