Literature DB >> 16332437

Discovery of potent, selective, and orally bioavailable pyridone-based dipeptidyl peptidase-4 inhibitors.

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

Abstract

anti-Substituted beta-methylphenylalanine derived amides have been shown to be potent DPP-IV inhibitors exhibiting excellent selectivity over both DPP8 and DPP9. The optimized compound exhibited good pharmacokinetic profiles in three preclinical species.

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Year:  2005        PMID: 16332437     DOI: 10.1016/j.bmcl.2005.11.052

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


  5 in total

1.  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

2.  Comprehensive analysis of the Co-structures of dipeptidyl peptidase IV and its inhibitor.

Authors:  Hiroyuki Nojima; Kazuhiko Kanou; Genki Terashi; Mayuko Takeda-Shitaka; Gaku Inoue; Koichiro Atsuda; Chihiro Itoh; Chie Iguchi; Hajime Matsubara
Journal:  BMC Struct Biol       Date:  2016-08-05

3.  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.  Fibroblast activation protein (FAP) as a novel metabolic target.

Authors:  Miguel Angel Sánchez-Garrido; Kirk M Habegger; Christoffer Clemmensen; Cassie Holleman; Timo D Müller; Diego Perez-Tilve; Pengyun Li; Archita S Agrawal; Brian Finan; Daniel J Drucker; Matthias H Tschöp; Richard D DiMarchi; Alexei Kharitonenkov
Journal:  Mol Metab       Date:  2016-07-16       Impact factor: 7.422

5.  Discovery of small-molecule enzyme activators by activity-based protein profiling.

Authors:  Bernard P Kok; Srijana Ghimire; Woojoo Kim; Shreyosree Chatterjee; Tyler Johns; Seiya Kitamura; Jerome Eberhardt; Daisuke Ogasawara; Janice Xu; Ara Sukiasyan; Sean M Kim; Cristina Godio; Julia M Bittencourt; Michael Cameron; Andrea Galmozzi; Stefano Forli; Dennis W Wolan; Benjamin F Cravatt; Dale L Boger; Enrique Saez
Journal:  Nat Chem Biol       Date:  2020-06-08       Impact factor: 15.040

  5 in total

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