Literature DB >> 21186796

Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV.

Zhiyuan Zhang1, Michael B Wallace, Jun Feng, Jeffrey A Stafford, Robert J Skene, Lihong Shi, Bumsup Lee, Kathleen Aertgeerts, Andy Jennings, Rongda Xu, Daniel B Kassel, Stephen W Kaldor, Marc Navre, David R Webb, Stephen L Gwaltney.   

Abstract

The discovery of two classes of heterocyclic dipeptidyl peptidase IV (DPP-4) inhibitors, pyrimidinones and pyrimidinediones, is described. After a single oral dose, these potent, selective, and noncovalent inhibitors provide sustained reduction of plasma DPP-4 activity and lowering of blood glucose in animal models of diabetes. Compounds 13a, 27b, and 27j were selected for development.

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Year:  2010        PMID： 21186796     DOI： 10.1021/jm101016w

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  10 in total

1.  Add-on treatment with teneligliptin ameliorates glucose fluctuations and improves glycemic control index in Japanese patients with type 2 diabetes on insulin therapy.

Authors:  Seiichi Tanaka; Kunihiro Suzuki; Chie Aoki; Mai Niitani; Kanako Kato; Takanori Tomotsune; Yoshimasa Aso
Journal:  Diabetes Technol Ther       Date:  2014-08-21       Impact factor: 6.118

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.  The Potential Role of Cyclopeptides from Pseudostellaria heterophylla, Linum usitatissimum and Drymaria diandra, and Peptides Derived from Heterophyllin B as Dipeptidyl Peptidase IV Inhibitors for the Treatment of Type 2 Diabetes: An In Silico Study.

Authors:  Hui-Jun Liao; Jason T C Tzen
Journal:  Metabolites       Date:  2022-04-24

4.  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

5.  Trelagliptin (SYR-472, Zafatek), Novel Once-Weekly Treatment for Type 2 Diabetes, Inhibits Dipeptidyl Peptidase-4 (DPP-4) via a Non-Covalent Mechanism.

Authors:  Charles E Grimshaw; Andy Jennings; Ruhi Kamran; Hikaru Ueno; Nobuhiro Nishigaki; Takuo Kosaka; Akiyoshi Tani; Hiroki Sano; Yoshinobu Kinugawa; Emiko Koumura; Lihong Shi; Koji Takeuchi
Journal:  PLoS One       Date:  2016-06-21       Impact factor: 3.240

6.  Comparative Binding Analysis of Dipeptidyl Peptidase IV (DPP-4) with Antidiabetic Drugs - An Ab Initio Fragment Molecular Orbital Study.

Authors:  Sundaram Arulmozhiraja; Naoya Matsuo; Erika Ishitsubo; Seiji Okazaki; Hitoshi Shimano; Hiroaki Tokiwa
Journal:  PLoS One       Date:  2016-11-10       Impact factor: 3.240

7.  A comparative study of the binding properties, dipeptidyl peptidase-4 (DPP-4) inhibitory activity and glucose-lowering efficacy of the DPP-4 inhibitors alogliptin, linagliptin, saxagliptin, sitagliptin and vildagliptin in mice.

Authors:  Joel P Berger; Ranabir SinhaRoy; Alessandro Pocai; Theresa M Kelly; Giovanna Scapin; Ying-Duo Gao; Kelly Ann D Pryor; Joseph K Wu; George J Eiermann; Shiyao S Xu; Xiaoping Zhang; Daniel A Tatosian; Ann E Weber; Nancy A Thornberry; Richard D Carr
Journal:  Endocrinol Diabetes Metab       Date:  2017-11-24

8.  Discovery of Novel DPP-IV Inhibitors as Potential Candidates for the Treatment of Type 2 Diabetes mellitus Predicted by 3D QSAR Pharmacophore Models, Molecular Docking and de novo Evolution.

Authors:  Azizullo Musoev; Sodik Numonov; Zhuhong You; Hongwei Gao
Journal:  Molecules       Date:  2019-08-07       Impact factor: 4.411

9.  tert-Butyl 4-{[2-amino-4-(2-hy-droxy-phen-yl)pyrimidin-5-yl]meth-yl}piperazine-1-carboxyl-ate.

Authors:  Nilesh N Gajera; Mukesh C Patel; Mukesh M Jotani; Edward R T Tiekink
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-09-21

10.  Antitubercular 2-Pyrazolylpyrimidinones: Structure-Activity Relationship and Mode-of-Action Studies.

Authors:  Candice Soares de Melo; Vinayak Singh; Alissa Myrick; Sandile B Simelane; Dale Taylor; Christel Brunschwig; Nina Lawrence; Dirk Schnappinger; Curtis A Engelhart; Anuradha Kumar; Tanya Parish; Qin Su; Timothy G Myers; Helena I M Boshoff; Clifton E Barry; Frederick A Sirgel; Paul D van Helden; Kirsteen I Buchanan; Tracy Bayliss; Simon R Green; Peter C Ray; Paul G Wyatt; Gregory S Basarab; Charles J Eyermann; Kelly Chibale; Sandeep R Ghorpade
Journal:  J Med Chem       Date:  2021-01-04       Impact factor: 7.446
  10 in total

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