Nitta_2008_Bioorg.Med.Chem.Lett_18_5435

Reference

Title : (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 - Nitta_2008_Bioorg.Med.Chem.Lett_18_5435
Author(s) : Nitta A , Fujii H , Sakami S , Nishimura Y , Ohyama T , Satoh M , Nakaki J , Satoh S , Inada C , Kozono H , Kumagai H , Shimamura M , Fukazawa T , Kawai H
Ref : Bioorganic & Medicinal Chemistry Lett , 18 :5435 , 2008
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.

PubMedSearch : Nitta_2008_Bioorg.Med.Chem.Lett_18_5435
PubMedID: 18819797

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Nitta A, Fujii H, Sakami S, Nishimura Y, Ohyama T, Satoh M, Nakaki J, Satoh S, Inada C, Kozono H, Kumagai H, Shimamura M, Fukazawa T, Kawai H (2008)
(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
Bioorganic & Medicinal Chemistry Lett 18 :5435

Nitta A, Fujii H, Sakami S, Nishimura Y, Ohyama T, Satoh M, Nakaki J, Satoh S, Inada C, Kozono H, Kumagai H, Shimamura M, Fukazawa T, Kawai H (2008)
Bioorganic & Medicinal Chemistry Lett 18 :5435