Literature DB >> 25147615

Discovery of Imigliptin, a Novel Selective DPP-4 Inhibitor for the Treatment of Type 2 Diabetes.

Chutian Shu1, Hu Ge2, Michael Song1, Jyun-Hong Chen1, Huimin Zhou1, Qu Qi1, Feng Wang1, Xifeng Ma1, Xiaolei Yang1, Genyan Zhang1, Yanwei Ding1, Dapeng Zhou1, Peng Peng1, Cheng-Kon Shih3, Jun Xu2, Frank Wu3.   

Abstract

We report our discovery of a novel series of potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. Starting from a lead identified by scaffold-hopping approach, our discovery and development efforts were focused on exploring structure-activity relationships, optimizing pharmacokinetic profile, improving in vitro and in vivo efficacy, and evaluating safety profile. The selected candidate, Imigliptin, is now undergoing clinical trial.

Entities:  

Keywords:  Diabetes; OGTT; dipeptidyl peptidase IV (DPP-4); imigliptin; inhibitor; pyridinylimidazolone; scaffold-hopping

Year:  2014        PMID： 25147615      PMCID： PMC4137375          DOI： 10.1021/ml5001905

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  8 in total

Review 1.  Biochemical properties of recombinant prolyl dipeptidases DPP-IV and DPP8.

Authors:  Xin Chen
Journal:  Adv Exp Med Biol       Date:  2006       Impact factor: 2.622

Review 2.  Profound methyl effects in drug discovery and a call for new C-H methylation reactions.

Authors:  Heike Schönherr; Tim Cernak
Journal:  Angew Chem Int Ed Engl       Date:  2013-10-22       Impact factor: 15.336

3.  Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9.

Authors:  George R Lankas; Barbara Leiting; Ranabir Sinha Roy; George J Eiermann; Maria G Beconi; Tesfaye Biftu; Chi-Chung Chan; Scott Edmondson; William P Feeney; Huaibing He; Dawn E Ippolito; Dooseop Kim; Kathryn A Lyons; Hyun O Ok; Reshma A Patel; Aleksandr N Petrov; Kelly Ann Pryor; Xiaoxia Qian; Leah Reigle; Andrea Woods; Joseph K Wu; Dennis Zaller; Xiaoping Zhang; Lan Zhu; Ann E Weber; Nancy A Thornberry
Journal:  Diabetes       Date:  2005-10       Impact factor: 9.461

4.  (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Authors:  Dooseop Kim; Liping Wang; Maria Beconi; George J Eiermann; Michael H Fisher; Huaibing He; Gerard J Hickey; Jennifer E Kowalchick; Barbara Leiting; Kathryn Lyons; Frank Marsilio; Margaret E McCann; Reshma A Patel; Aleksandr Petrov; Giovanna Scapin; Sangita B Patel; Ranabir Sinha Roy; Joseph K Wu; Matthew J Wyvratt; Bei B Zhang; Lan Zhu; Nancy A Thornberry; Ann E Weber
Journal:  J Med Chem       Date:  2005-01-13       Impact factor: 7.446

Review 5.  Dipeptidyl peptidase IV and its inhibitors: therapeutics for type 2 diabetes and what else?

Authors:  Lucienne Juillerat-Jeanneret
Journal:  J Med Chem       Date:  2013-10-24       Impact factor: 7.446

Review 6.  Dipeptidyl peptidase IV (DPP IV) and related molecules in type 2 diabetes.

Authors:  Peter R Flatt; Clifford J Bailey; Brian D Green
Journal:  Front Biosci       Date:  2008-05-01

Review 7.  National, regional, and global trends in fasting plasma glucose and diabetes prevalence since 1980: systematic analysis of health examination surveys and epidemiological studies with 370 country-years and 2·7 million participants.

Authors:  Goodarz Danaei; Mariel M Finucane; Yuan Lu; Gitanjali M Singh; Melanie J Cowan; Christopher J Paciorek; John K Lin; Farshad Farzadfar; Young-Ho Khang; Gretchen A Stevens; Mayuree Rao; Mohammed K Ali; Leanne M Riley; Carolyn A Robinson; Majid Ezzati
Journal:  Lancet       Date:  2011-06-24       Impact factor: 79.321

8.  Globalization of diabetes: the role of diet, lifestyle, and genes.

Authors:  Frank B Hu
Journal:  Diabetes Care       Date:  2011-06       Impact factor: 19.112
  8 in total
  5 in total

1.  Synthesis of New DPP-4 Inhibitors Based on a Novel Tricyclic Scaffold.

Authors:  Carolin Schwehm; Jin Li; Hongmei Song; Xiao Hu; Barrie Kellam; Michael J Stocks
Journal:  ACS Med Chem Lett       Date:  2015-01-13       Impact factor: 4.345

2.  Scaffold-Hopping of Aurones: 2-Arylideneimidazo[1,2-a]pyridinones as Topoisomerase IIα-Inhibiting Anticancer Agents.

Authors:  Garima Priyadarshani; Anmada Nayak; Suyog M Amrutkar; Sarita Das; Sankar K Guchhait; Chanakya N Kundu; Uttam C Banerjee
Journal:  ACS Med Chem Lett       Date:  2016-09-20       Impact factor: 4.345

3.  Design, synthesis and biological evaluation of benzimidazole-rhodanine conjugates as potent topoisomerase II inhibitors.

Authors:  Penghui Li; Wenjin Zhang; Hong Jiang; Yongliang Li; Changzhi Dong; Huixiong Chen; Kun Zhang; Zhiyun Du
Journal:  Medchemcomm       Date:  2018-06-02       Impact factor: 3.597

4.  Bioactive Molecules and Their Mechanisms of Action.

Authors:  Dongdong Wang; Elke Heiss; Karel Šmejkal; Atanas G Atanasov
Journal:  Molecules       Date:  2019-10-18       Impact factor: 4.411

5.  Dipeptidyl-Peptidase-IV Inhibitors, Imigliptin and Alogliptin, Improve Beta-Cell Function in Type 2 Diabetes.

Authors:  Xu Liu; Yang Liu; Hongzhong Liu; Haiyan Li; Jianhong Yang; Pei Hu; Xinhua Xiao; Dongyang Liu
Journal:  Front Endocrinol (Lausanne)       Date:  2021-09-20       Impact factor: 5.555
  5 in total

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