Literature DB >> 14980678

Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.

Charles G Caldwell1, Ping Chen, Jiafang He, Emma R Parmee, Barbara Leiting, Frank Marsilio, Reshma A Patel, Joseph K Wu, George J Eiermann, Aleksandr Petrov, Huaibing He, Kathryn A Lyons, Nancy A Thornberry, Ann E Weber.   

Abstract

Amides derived from fluorinated pyrrolidines and 4-substituted cyclohexylglycine analogues have been prepared and evaluated as inhibitors of dipeptidyl dipeptidase IV (DP-IV). Analogues which incorporated (S)-3-fluoropyrrolidine showed good selectivity for DP-IV over quiescent cell proline dipeptidase (QPP). Compound 48 had good pharmacokinetic properties and was orally active in an oral glucose tolerance test in lean mice.

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Year:  2004        PMID: 14980678     DOI: 10.1016/j.bmcl.2003.12.040

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  3D-QSAR studies on fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors by CoMFA and CoMSIA.

Authors:  Juan Zeng; Guixia Liu; Yun Tang; Hualiang Jiang
Journal:  J Mol Model       Date:  2007-07-06       Impact factor: 1.810

2.  The vicinal difluoro motif: The synthesis and conformation of erythro- and threo- diastereoisomers of 1,2-difluorodiphenylethanes, 2,3-difluorosuccinic acids and their derivatives.

Authors:  David O'Hagan; Henry S Rzepa; Martin Schüler; Alexandra M Z Slawin
Journal:  Beilstein J Org Chem       Date:  2006-10-02       Impact factor: 2.883

Review 3.  Kitamura Electrophilic Fluorination Using HF as a Source of Fluorine.

Authors:  Jianlin Han; Greg Butler; Hiroki Moriwaki; Hiroyuki Konno; Vadim A Soloshonok; Tsugio Kitamura
Journal:  Molecules       Date:  2020-04-30       Impact factor: 4.411

  3 in total

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