Literature DB >> 19833514

The design of potent and selective inhibitors of DPP-4: optimization of ADME properties by amide replacements.

Sonja Nordhoff1, Stephan Bulat, Silvia Cerezo-Gálvez, Oliver Hill, Barbara Hoffmann-Enger, Meritxell López-Canet, Claudia Rosenbaum, Christian Rummey, Meinolf Thiemann, Victor G Matassa, Paul J Edwards, Achim Feurer.   

Abstract

For a series of beta-homophenylalanine based inhibitors of dipeptidyl peptidase IV ADME properties were improved by the incorporation of amide replacements. These efforts led to a novel series of potent and selective inhibitors of DPP-4 that exhibit an attractive pharmacokinetic profile and show excellent efficacy in an animal model of diabetes.

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Year:  2009        PMID: 19833514     DOI: 10.1016/j.bmcl.2009.09.078

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


  4 in total

Review 1.  Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.

Authors:  Shikha Kumari; Angelica V Carmona; Amit K Tiwari; Paul C Trippier
Journal:  J Med Chem       Date:  2020-08-04       Impact factor: 7.446

2.  Identification of diverse dipeptidyl peptidase IV inhibitors via structure-based virtual screening.

Authors:  Cui Li; Weiqiang Lu; Chunhua Lu; Wen Xiao; Xu Shen; Jin Huang; Guixia Liu; Yun Tang
Journal:  J Mol Model       Date:  2012-03-30       Impact factor: 1.810

3.  Design, synthesis and cytotoxic evaluation of a library of oxadiazole-containing hybrids.

Authors:  Cristián M Camacho; Marianela G Pizzio; David L Roces; Dora B Boggián; Ernesto G Mata; Yanina Bellizzi; Elizabeth Barrionuevo; Viviana C Blank; Leonor P Roguin
Journal:  RSC Adv       Date:  2021-09-06       Impact factor: 4.036

4.  Design, Synthesis and Biological Evaluation of Neogliptin, a Novel 2-Azabicyclo[2.2.1]heptane-Based Inhibitor of Dipeptidyl Peptidase-4 (DPP-4).

Authors:  Ivan O Maslov; Tatiana V Zinevich; Olga G Kirichenko; Mikhail V Trukhan; Sergey V Shorshnev; Natalya O Tuaeva; Maxim A Gureev; Amelia D Dahlén; Yuri B Porozov; Helgi B Schiöth; Vladimir M Trukhan
Journal:  Pharmaceuticals (Basel)       Date:  2022-02-22
  4 in total

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