775353-65-6Relevant academic research and scientific papers
THIAZOLIDINE DERIVATIVES AND METHODS FOR THE PREPARATION THEREOF
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Page/Page column 65, (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.
Potent and selective proline derived dipeptidyl peptidase IV inhibitors
Edmondson, Scott D.,Mastracchio, Anthony,Beconi, Maria,Colwell Jr., Lawrence F.,Habulihaz, Bahanu,He, Huaibing,Kumar, Sanjeev,Leiting, Barbara,Lyons, Kathryn A.,Mao, Ann,Marsilio, Frank,Patel, Reshma A.,Wu, Joseph K.,Zhu, Lan,Thornberry, Nancy A.,Weber, Ann E.,Parmee, Emma R.
, p. 5151 - 5155 (2007/10/03)
In-house screening of the Merck sample collection identified proline derived homophenylalanine 3 as a DPP-IV inhibitor with modest potency (DPP-IV IC50 = 1.9 μM). Optimization of 3 led to compound 37, which is among the most potent and selectiv
