1041609-60-2Relevant academic research and scientific papers
Discovery of β-aminoacyl containing thiazolidine derivatives as potent and selective dipeptidyl peptidase IV inhibitors
Park, Woul Seong,Kang, Seung Kyu,Jun, Mi Ae,Shin, Mi Sik,Kim, Ki Young,Rhee, Sang Dal,Bae, Myung Ae,Kim, Min Sun,Kim, Kwang Rok,Kang, Nam Sook,Yoo, Sung-Eun,Lee, Jie Oh,Song, Dong Hyun,Silinski, Peter,Schneider, Stephen Edward,Ahn, Jin Hee,Kim, Sung Soo
scheme or table, p. 1366 - 1370 (2011/04/16)
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 IC50 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.
THIAZOLIDINE DERIVATIVES AND METHODS FOR THE PREPARATION THEREOF
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Page/Page column 87, (2010/03/31)
The present invention relates to novel 2-carbonyl-3-acyl-1,3-thiazolidines having a β-amino group on the acyl chain, in free, prodrug form or pharmaceutically acceptable salt thereof, including their enantiomers, diastereomers and racemates, as efficient inhibitors against DPP-IV. The invention further relates to the pharmaceutical compositions comprising the disclosed compounds. The present invention also relates to methods for preparing the disclosed compounds and for treating DPP-IV-mediated diseases.
