Literature DB >> 16919457

Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors.

Jinyou Xu1, Lan Wei, Robert J Mathvink, Scott D Edmondson, George J Eiermann, Huaibing He, Joseph F Leone, Barbara Leiting, Kathryn A Lyons, Frank Marsilio, Reshma A Patel, Sangita B Patel, Aleksandr Petrov, Giovanna Scapin, Joseph K Wu, Nancy A Thornberry, Ann E Weber.   

Abstract

A novel series of oxadiazole based amides have been shown to be potent DPP-4 inhibitors. The optimized compound 43 exhibited excellent selectivity over a variety of DPP-4 homologs.

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Year:  2006        PMID: 16919457     DOI: 10.1016/j.bmcl.2006.07.061

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


  4 in total

1.  Ligand deconstruction: Why some fragment binding positions are conserved and others are not.

Authors:  Dima Kozakov; David R Hall; Stefan Jehle; Sefan Jehle; Lingqi Luo; Stefan O Ochiana; Elizabeth V Jones; Michael Pollastri; Karen N Allen; Adrian Whitty; Sandor Vajda
Journal:  Proc Natl Acad Sci U S A       Date:  2015-04-27       Impact factor: 11.205

2.  CoMFA and CoMSIA of diverse pyrrolidine analogues as dipeptidyl peptidase IV inhibitors: active site requirements.

Authors:  Vanangamudi Murugesan; Nidhi Sethi; Yenamandra S Prabhakar; Seturam B Katti
Journal:  Mol Divers       Date:  2010-08-25       Impact factor: 2.943

3.  Synthesis, X-ray diffraction analysis, quantum chemical studies and α-amylase inhibition of probenecid derived S-alkylphthalimide-oxadiazole-benzenesulfonamide hybrids.

Authors:  Bilal Ahmad Khan; Syeda Shamila Hamdani; Muhammad Naeem Ahmed; Shahid Hameed; Muhammad Ashfaq; Ahmed M Shawky; Mahmoud A A Ibrahim; Peter A Sidhom
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756

4.  Predicting the DPP-IV inhibitory activity pIC₅₀ based on their physicochemical properties.

Authors:  Tianhong Gu; Xiaoyan Yang; Minjie Li; Milin Wu; Qiang Su; Wencong Lu; Yuhui Zhang
Journal:  Biomed Res Int       Date:  2013-06-20       Impact factor: 3.411

  4 in total

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