4-Phenylpyridine glucagon receptor antagonists: synthetic approaches to the sterically hindered chiral hydroxy group

2002 ◽  
Vol 43 (25) ◽  
pp. 4455-4458 ◽  
Author(s):  
Gaetan H. Ladouceur ◽  
James H. Cook ◽  
Elizabeth M. Doherty ◽  
Dierk Giebel ◽  
William R. Schoen
Keyword(s):  
Hydroxy Group ◽  
Receptor Antagonists ◽  
Glucagon Receptor ◽  
Sterically Hindered ◽  
Synthetic Approaches

scholarly journals Stable Bicyclic Functionalized Nitroxides: The Synthesis of Derivatives of Aza-nortropinone–5-Methyl-3-oxo-6,8-diazabicyclo[3.2.1]-6-octene 8-oxyls

Molecules ◽  
2021 ◽  
Vol 26 (10) ◽  
pp. 3050
Author(s):  
Larisa N. Grigor’eva ◽  
Alexsei Ya. Tikhonov ◽  
Konstantin A. Lomanovich ◽  
Dmitrii G. Mazhukin
Keyword(s):  
Hydroxy Group ◽  
Lead Dioxide ◽  
Nitroxyl Radicals ◽  
Design And Development ◽  
New Class ◽  
Oxidation Of Alcohols ◽  
Oxidative Transformations ◽  
Sterically Hindered ◽  
Synthetic Approaches ◽  
Derivatives Of

In recent decades, bicyclic nitroxyl radicals have caught chemists’ attention as selective catalysts for the oxidation of alcohols and amines and as additives and mediators in directed C-H oxidative transformations. In this regard, the design and development of synthetic approaches to new functional bicyclic nitroxides is a relevant and important issue. It has been reported that imidazo[1,2-b]isoxazoles formed during the condensation of acetylacetone with 2-hydroxyaminooximes having a secondary hydroxyamino group are recyclized under mild basic catalyzed conditions to 8-hydroxy-5-methyl-3-oxo-6,8-diazabicyclo[3.2.1]-6-octenes. The latter, containing a sterically hindered cyclic N-hydroxy group, upon oxidation with lead dioxide in acetone, virtually quantitatively form stable nitroxyl bicyclic radicals of a new class, which are derivatives of both 2,2,6,6-tetramethyl-4-oxopiperidine-1-oxyl (TEMPON) and 3-imidazolines.

scholarly journals Synthesis and Anti‐Diabetic Activity of Novel Biphenylsulfonamides as Glucagon Receptor Antagonists

2021 ◽  
Author(s):  
Chang‐Yong Lee ◽  
Hojung Choi ◽  
Eun‐Young Park ◽  
Thi‐Thao‐Linh Nguyen ◽  
Han‐Joo Maeng ◽  
...  
Keyword(s):  
Receptor Antagonists ◽  
Glucagon Receptor

Proglucagon-Derived Peptides: Mechanisms of Action and Therapeutic Potential

Physiology ◽  
2005 ◽  
Vol 20 (5) ◽  
pp. 357-365 ◽  
Author(s):  
Elaine M Sinclair ◽  
Daniel J. Drucker
Keyword(s):  
Type 2 Diabetes ◽  
Human Disease ◽  
Clinical Relevance ◽  
Therapeutic Potential ◽  
Mechanisms Of Action ◽  
Receptor Antagonists ◽  
Glucagon Receptor ◽  
Receptor Agonists ◽  
Glucagon Like Peptide

Glucagon is used for the treatment of hypoglycemia, and glucagon receptor antagonists are under development for the treatment of type 2 diabetes. Moreover, glucagon-like peptide (GLP)-1 and GLP-2 receptor agonists appear to be promising therapies for the treatment of type 2 diabetes and intestinal disorders, respectively. This review discusses the physiological, pharmacological, and therapeutic actions of the proglucagon-derived peptides, with an emphasis on clinical relevance of the peptides for the treatment of human disease.

ChemInform Abstract: Substituted Imidazoles a Glucagon Receptor Antagonists.

ChemInform ◽  
2010 ◽  
Vol 33 (5) ◽  
pp. no-no
Author(s):  
Linda L. Chang ◽  
et al. et al.
Keyword(s):  
Receptor Antagonists ◽  
Glucagon Receptor

Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core

2011 ◽  
Vol 21 (1) ◽  
pp. 76-81 ◽  
Author(s):  
Dong-Ming Shen ◽  
Edward J. Brady ◽  
Mari R. Candelore ◽  
Qing Dallas-Yang ◽  
Victor D.-H. Ding ◽  
...  
Keyword(s):  
Receptor Antagonists ◽  
Glucagon Receptor ◽  
Orally Active

Direct observation (NMR) of the efficacy of glucagon receptor antagonists in murine liver expressing the human glucagon receptor

2006 ◽  
Vol 14 (5) ◽  
pp. 1506-1517 ◽  
Author(s):  
Sheila M. Cohen ◽  
Joseph L. Duffy ◽  
Corin Miller ◽  
Brian A. Kirk ◽  
Mari Rios Candelore ◽  
...  
Keyword(s):  
Direct Observation ◽  
Receptor Antagonists ◽  
Glucagon Receptor ◽  
Murine Liver

Discovery of novel, potent, and orally active spiro-urea human glucagon receptor antagonists

2005 ◽  
Vol 15 (20) ◽  
pp. 4564-4569 ◽  
Author(s):  
Dong-Ming Shen ◽  
Fengqi Zhang ◽  
Edward J. Brady ◽  
Mari Rios Candelore ◽  
Qing Dallas-Yang ◽  
...  
Keyword(s):  
Receptor Antagonists ◽  
Glucagon Receptor ◽  
Orally Active

Potent, orally absorbed glucagon receptor antagonists

1999 ◽  
Vol 9 (5) ◽  
pp. 641-646 ◽  
Author(s):  
Stephen E. de Laszlo ◽  
Candice Hacker ◽  
Bing Li ◽  
Dooseop Kim ◽  
Malcolm MacCoss ◽  
...  
Keyword(s):  
Receptor Antagonists ◽  
Glucagon Receptor
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