Synthesis and pharmacological characterization of potent selective and orally bioavailable isoindoline class dipeptidyl peptidase IV inhibitors

摘要

Focused structure-activity relationships of isoindoline class DPP-IV inhibitors have led to the discovery of >4b as a highly selective, potent inhibitor of DPP-IV. In vivo studies in Wistar/ST rats showed that >4b was converted into the strongly active metabolite >4l in high yield, resulting in good in vivo efficacy for antihyperglycemic activity.