Concepedia

Designing glucokinase activators with reduced hypoglycemia risk: discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4-yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus

Jeffrey A. Pfefferkorn, Angel Guzmán-Pérez, Peter J. Oates, John Litchfield, Gary E. Aspnes, Arindrajit Basak, John W. Benbow, Martin A. Berliner, Jianwei Bian, Chulho Choi,

MedChemComm · 2011 · 68 citations · 20 references

DOI

Concepts

Abstract

Optimization of a substituted 2-methylbenzofuran series led to the discovery of N , N -dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4-yloxy)pyrimidine-2-carboxamide as a glucokinase activator for treating Type 2 diabetes.

References

20

Enzyme kinetics; behavior and analysis of rapid equilibrium and steady state enzyme systems

International Journal of Biochemistry · 1994 · 3K citations

, , +16

Allosteric Activators of Glucokinase: Potential Role in Diabetes Therapy

Joseph Grimsby, Ramakanth Sarabu, Wendy L. Corbett et al. · Science · 2003 · 537 citations

, , +17

Structural Basis for Allosteric Regulation of the Monomeric Allosteric Enzyme Human Glucokinase

Kenji Kamata, Morihiro Mitsuya, T. Nishimura et al. · Structure · 2004 · 503 citations · Full text

, , +16

Significantly Improved Method for the Pd‐Catalyzed Coupling of Phenols with Aryl Halides: Understanding Ligand Effects

Carlos H. Burgos, Timothy E. Barder, Xiaohua Huang et al. · Angewandte Chemie International Edition · 2006 · 342 citations

, , +11

Glucokinase Is the Likely Mediator of Glucosensing in Both Glucose-Excited and Glucose-Inhibited Central Neurons

Ambrose A. Dunn-Meynell, Vanessa H. Routh, Ling Kang et al. · Diabetes · 2002 · 308 citations · Full text

, , +11