(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
作者:Aiko Nitta、Hideaki Fujii、Satoshi Sakami、Yutaka Nishimura、Tomofumi Ohyama、Mikiya Satoh、Junko Nakaki、Shiho Satoh、Chifumi Inada、Hideki Kozono、Hiroki Kumagai、Masahiro Shimamura、Tominaga Fukazawa、Hideki Kawai
DOI:10.1016/j.bmcl.2008.09.042
日期:2008.10
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
合成了一系列新颖的3-
氨基-N-(4-芳基-1,1-二氧
噻吩-4-基)丁酰胺和3-
氨基-N-(4-芳基
四氢吡喃-4-基)丁酰胺并评估为
二肽基肽酶IV (
DPP-IV)
抑制剂。掺入6-取代的
苯并噻唑基团的衍
生物显示出强效的
DPP-IV抑制活性。(3R)-3-
氨基-4-(2,4,5-三
氟苯基)-N- 4- [6-(2-甲氧基乙氧基)
苯并噻唑-2-基]
四氢吡喃-4-基}丁酰胺的口服给药( 12u)在
口服葡萄糖耐量试验中降低了血糖偏移。