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Discovery of β-aminoacyl containing thiazolidine derivatives as potent and selective dipeptidyl peptidase IV inhibitors

Park, WS., Kang, SK., Jun, MA., Shin, MS., Kim, KY., Rhee, SD., Bae, MA., Kim, MS., Kim, KR., Kang, NS., Yoo, SE., Lee, JO., Song, DH., Silinski, P., Schneider, SE., Ahn, JH., & Kim, SS. (2011). Discovery of β-aminoacyl containing thiazolidine derivatives as potent and selective dipeptidyl peptidase IV inhibitors. Bioorganic and Medicinal Chemistry Letters, 21(5), 1366-1370. https://doi.org/10.1016/j.bmcl.2011.01.041

Abstract

A series of β-aminoacyl containing thiazolidine derivatives was synthesized and evaluated for their ability to inhibit DPP-IV. Several thiazolidine derivatives with an acid moiety were found to be potent DPP-IV inhibitors. Among them, compound 2da is the most active in this series with an IC(50) value of 1 nM, and it showed excellent selectivity over DPP-IV related enzymes including DPP-2, DPP-8, and DPP-9. Compound 2da is chemically and metabolically stable, and showed no CYP inhibition, hERG binding or cytotoxicity. Compound 2db, an ester prodrug of 2da, showed good in vivo DPP-IV inhibition after oral administration in rat and dog models.

10.1016/j.bmcl.2011.01.041

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