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

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, (3 R )-3-amino- N -(4-(4-phenylthiazol-2-yl)-tetrahydro-2 H -thiopyran-4-yl)-4-(2,4,5-trifluorophenyl)butanamide 1,1-dioxide ( 30 ) reduced blood glucose excursion in an oral glucose tolerance test by oral administration.