Literature DB >> 10201821

Potent, orally absorbed glucagon receptor antagonists.

S E de Laszlo1, C Hacker, B Li, D Kim, M MacCoss, N Mantlo, J V Pivnichny, L Colwell, G E Koch, M A Cascieri, W K Hagmann.   

Abstract

The SAR of 2-pyridyl-3,5-diaryl pyrroles, ligands of the human glucagon receptor and inhibitors of p38 kinase, were investigated. This effort resulted in the identification of 2-(4-pyridyl)-5-(4-chlorophenyl)-3-(5-bromo-2-propyloxyphenyl)pyrr ole 49 (L-168,049), a potent (Kb = 25 nM), selective antagonist of glucagon.

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Year:  1999        PMID: 10201821     DOI: 10.1016/s0960-894x(99)00081-5

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


  13 in total

Review 1.  Current advances in the synthesis and biological potencies of tri- and tetra-substituted 1H-imidazoles.

Authors:  Majid M Heravi; Mansoureh Daraie; Vahideh Zadsirjan
Journal:  Mol Divers       Date:  2015-04-12       Impact factor: 2.943

2.  Paracrine Interactions within the Pancreatic Islet Determine the Glycemic Set Point.

Authors:  Rayner Rodriguez-Diaz; R Damaris Molano; Jonathan R Weitz; Midhat H Abdulreda; Dora M Berman; Barbara Leibiger; Ingo B Leibiger; Norma S Kenyon; Camillo Ricordi; Antonello Pileggi; Alejandro Caicedo; Per-Olof Berggren
Journal:  Cell Metab       Date:  2018-03-06       Impact factor: 27.287

3.  Glucagon signaling modulates sweet taste responsiveness.

Authors:  Amanda E T Elson; Cedrick D Dotson; Josephine M Egan; Steven D Munger
Journal:  FASEB J       Date:  2010-06-14       Impact factor: 5.191

4.  Site Specific Interaction Between TiO2 Nanoparticles and Phenanthrimidazole-A First Principles Quantum Mechanical Study.

Authors:  Jayaraman Jayabharathi; Periyasamy Ramanathan; Chockalingam Karunakaran; Venugopal Thanikachalam
Journal:  J Fluoresc       Date:  2015-06-26       Impact factor: 2.217

5.  Photoinduced electron transfer from phenanthrimidazole to magnetic nanoparticles.

Authors:  J Jayabharathi; A Arunpandiyan; V Thanikachalam; P Ramanathan
Journal:  J Fluoresc       Date:  2015-01-17       Impact factor: 2.217

6.  Wells-Dawson heteropolyacid supported on silica: a highly efficient catalyst for synthesis of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazoles.

Authors:  Ali Reza Karimi; Zahra Alimohammadi; Mostafa M Amini
Journal:  Mol Divers       Date:  2009-10-29       Impact factor: 2.943

7.  Rh(I)-catalyzed arylation of heterocycles via C-H bond activation: expanded scope through mechanistic insight.

Authors:  Jared C Lewis; Ashley M Berman; Robert G Bergman; Jonathan A Ellman
Journal:  J Am Chem Soc       Date:  2008-02-02       Impact factor: 15.419

8.  Supported heteropoly acids offering strong option for efficient and cleaner processing for the synthesis of imidazole derivatives under solvent-free condition.

Authors:  Ezzat Rafiee; Houri Mahdavi; Mohammad Joshaghani
Journal:  Mol Divers       Date:  2010-01-26       Impact factor: 2.943

9.  Allosteric modulators of class B G-protein-coupled receptors.

Authors:  Sam R J Hoare
Journal:  Curr Neuropharmacol       Date:  2007-09       Impact factor: 7.363

10.  2-(4-Meth-oxy-phen-yl)-1-pentyl-4,5-di-phenyl-1H-imidazole.

Authors:  Jim Simpson; Shaaban K Mohamed; Adel A Marzouk; Avtandil H Talybov; Antar A Abdelhamid
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-12-05
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