Novel series of 3-amino-N-(4-aryl-1, 1-dioxothian-4-yl) butanamides as potent and selective dipeptidyl peptidase IV inhibitors

…, H Fujii, S Sakami, M Satoh, J Nakaki, S Satoh…

Index: Nitta, Aiko; Fujii, Hideaki; Sakami, Satoshi; Satoh, Mikiya; Nakaki, Junko; Satoh, Shiho; Kumagai, Hiroki; Kawai, Hideki Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 23 p. 7036 - 7040

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Citation Number: 10

Abstract

A series of novel 3-amino-N-(4-aryl-1, 1-dioxothian-4-yl) butanamides were investigated as dipeptidyl peptidase IV (DPP-4) inhibitors. Introduction of a 4-phenylthiazol-2-yl group showed highly potent DPP-4 inhibitory activity. Among various derivatives,(3R)-3-amino-N- (4-(4-phenylthiazol-2-yl)-tetrahydro-2H-thiopyran-4-yl)-4-(2, 4, 5-trifluorophenyl) butanamide 1, 1-dioxide (30) reduced blood glucose excursion in an oral glucose tolerance test by ...