Literature DB >> 11814820

Discovery of 5-hydroxyalkyl-4-phenylpyridines as a new class of glucagon receptor antagonists.

Gaetan H Ladouceur1, James H Cook, Elizabeth M Doherty, William R Schoen, Margit L MacDougall, James N Livingston.   

Abstract

5-Hydroxyalkyl-4-phenylpyridines have been identified as a novel class of glucagon antagonists with potential utility for the treatment of diabetes. A lead structure with moderate activity was discovered through a high throughput screening assay. Structure-activity relationships led to the discovery of a potent antagonist, IC(50)=0.11 microM, more than 60-fold improvement over the lead structure.

Entities:  

Mesh:

Substances:

Year:  2002        PMID: 11814820     DOI: 10.1016/s0960-894x(01)00766-1

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


  2 in total

Review 1.  The alpha-cell as target for type 2 diabetes therapy.

Authors:  Mikkel Christensen; Jonatan I Bagger; Tina Vilsbøll; Filip K Knop
Journal:  Rev Diabet Stud       Date:  2011-11-10

2.  Recent Progress in the Use of Glucagon and Glucagon Receptor Antago-nists in the Treatment of Diabetes Mellitus.

Authors:  Mohamed Lotfy; Huba Kalasz; Gyorgy Szalai; Jaipaul Singh; Ernest Adeghate
Journal:  Open Med Chem J       Date:  2014-12-31
  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.