Literature DB >> 25815154

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

Carolin Schwehm1, Jin Li2, Hongmei Song2, Xiao Hu2, Barrie Kellam1, Michael J Stocks1.   

Abstract

A novel molecular scaffold has been synthesized, and its synthesis and incorporation into new analogues of biologically active molecules will be discussed. A comparison of the inhibitory activity of these compounds to the known type-2 diabetes compound (sitagliptin) against dipeptidyl peptidase-4 (DPP-4) will be shown.

Entities:  

Keywords:  1,2,4-triazole; Diabetes; crystal structure; dipeptyl peptidase VI (DPP-4) inhibitor; scaffold

Year:  2015        PMID： 25815154      PMCID： PMC4360159          DOI： 10.1021/ml500503n

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


  13 in total

1.  Conformer generation with OMEGA: learning from the data set and the analysis of failures.

Authors:  Paul C D Hawkins; Anthony Nicholls
Journal:  J Chem Inf Model       Date:  2012-11-12       Impact factor: 4.956

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

Authors:  Chutian Shu; Hu Ge; Michael Song; Jyun-Hong Chen; Huimin Zhou; Qu Qi; Feng Wang; Xifeng Ma; Xiaolei Yang; Genyan Zhang; Yanwei Ding; Dapeng Zhou; Peng Peng; Cheng-Kon Shih; Jun Xu; Frank Wu
Journal:  ACS Med Chem Lett       Date:  2014-06-16       Impact factor: 4.345

3.  Preparation and structural analysis of (±)-cis-ethyl 2-sulfanylidenedecahydro-1,6-naphthyridine-6-carboxylate and (±)-trans-ethyl 2-oxooctahydro-1H-pyrrolo[3,2-c]pyridine-5-carboxylate.

Authors:  Carolin Schwehm; William Lewis; Alexander J Blake; Barrie Kellam; Michael J Stocks
Journal:  Acta Crystallogr C Struct Chem       Date:  2014-11-19       Impact factor: 1.172

Review 4.  The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes.

Authors:  Daniel J Drucker; Michael A Nauck
Journal:  Lancet       Date:  2006-11-11       Impact factor: 79.321

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

6.  Reduced incretin effect in type 2 (non-insulin-dependent) diabetes.

Authors:  M Nauck; F Stöckmann; R Ebert; W Creutzfeldt
Journal:  Diabetologia       Date:  1986-01       Impact factor: 10.122

Review 7.  Glucagon-like peptide-1, a new hormone of the entero-insular axis.

Authors:  C Orskov
Journal:  Diabetologia       Date:  1992-08       Impact factor: 10.122

Review 8.  Dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes: focus on sitagliptin.

Authors:  G A Herman; P P Stein; N A Thornberry; J A Wagner
Journal:  Clin Pharmacol Ther       Date:  2007-03-28       Impact factor: 6.875

9.  Synthesis, biological activity, and three-dimensional quantitative structure-activity relationship model for a series of benzo[c]quinolizin-3-ones, nonsteroidal inhibitors of human steroid 5alpha-reductase 1.

Authors:  Ernesto G Occhiato; Alessandro Ferrali; Gloria Menchi; Antonio Guarna; Giovanna Danza; Alessandra Comerci; Rosa Mancina; Mario Serio; Gianni Garotta; Andrea Cavalli; Marco De Vivo; Maurizio Recanatini
Journal:  J Med Chem       Date:  2004-07-01       Impact factor: 7.446

10.  Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.

Authors:  Tesfaye Biftu; Ranabir Sinha-Roy; Ping Chen; Xiaoxia Qian; Dennis Feng; Jeffrey T Kuethe; Giovanna Scapin; Ying Duo Gao; Youwei Yan; Davida Krueger; Annette Bak; George Eiermann; Jiafang He; Jason Cox; Jacqueline Hicks; Kathy Lyons; Huaibing He; Gino Salituro; Sharon Tong; Sangita Patel; George Doss; Aleksandr Petrov; Joseph Wu; Shiyao Sherrie Xu; Charles Sewall; Xiaoping Zhang; Bei Zhang; Nancy A Thornberry; Ann E Weber
Journal:  J Med Chem       Date:  2014-04-02       Impact factor: 7.446
View more
  2 in total

1.  Computational Analysis of Gynura bicolor Bioactive Compounds as Dipeptidyl Peptidase-IV Inhibitor.

Authors:  Lina Rozano; Muhammad Redha Abdullah Zawawi; Muhamad Aizuddin Ahmad; Indu Bala Jaganath
Journal:  Adv Bioinformatics       Date:  2017-08-08

2.  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
  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.