Literature DB >> 20598534

Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes.

Robert P Brigance1, Wei Meng, Aberra Fura, Thomas Harrity, Aiying Wang, Robert Zahler, Mark S Kirby, Lawrence G Hamann.   

Abstract

Several pyrazolo-, triazolo-, and imidazolopyrimidines were synthesized and evaluated as inhibitors of DPP4. Of these three classes of compounds, the imidazolopyrimidines displayed the greatest potency and demonstrated excellent selectivity over the other dipeptidyl peptidases. SAR evaluation for these scaffolds was described as they may represent potential treatments for type 2 diabetes. Copyright 2010 Elsevier Ltd. All rights reserved.

Entities:  

Mesh：

Substances：

Year:  2010        PMID： 20598534     DOI： 10.1016/j.bmcl.2010.06.063

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


  3 in total

Review 1.  Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.

Authors:  Khalid Karrouchi; Smaail Radi; Youssef Ramli; Jamal Taoufik; Yahia N Mabkhot; Faiz A Al-Aizari; M'hammed Ansar
Journal:  Molecules       Date:  2018-01-12       Impact factor: 4.411

2.  Synthesis, structure and biological evaluation of ruthenium(III) complexes of triazolopyrimidines with anticancer properties.

Authors:  Marzena Fandzloch; Liliana Dobrzańska; Tomasz Jędrzejewski; Julia Jezierska; Joanna Wiśniewska; Iwona Łakomska
Journal:  J Biol Inorg Chem       Date:  2019-11-18       Impact factor: 3.358

3.  Synthesis of pyrazolopyrimidinones using a "one-pot" approach under microwave irradiation.

Authors:  Mark Kelada; John M D Walsh; Robert W Devine; Patrick McArdle; John C Stephens
Journal:  Beilstein J Org Chem       Date:  2018-05-28       Impact factor: 2.883
  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.