Discovery of novel 3,6-disubstituted 2-pyridinecarboxamide derivatives as GK activators.

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Mitsuya M, Kamata K, Bamba M, Watanabe H, Sasaki Y, Sasaki K, Ohyama S, Hosaka H, Nagata Y, Eiki J, Nishimura T

Discovery of novel 3,6-disubstituted 2-pyridinecarboxamide derivatives as GK activators.

Bioorg Med Chem Lett. 2009 May 15;19(10):2718-21. doi: 10.1016/j.bmcl.2009.03.137. Epub 2009 Mar 29.

PubMed ID

19362831 [ View in PubMed

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Abstract

A novel class of 3,6-disubstituted 2-pyridinecarboxamide derivatives was designed based on X-ray analysis of the 2-aminobenzamide lead class. Subsequent chemical modification led to the discovery of potent GK activators which eliminate potential toxicity concerns associated with an aniline group of the lead structure. Compound 7 demonstrated glucose lowering effect in a rat OGTT model.

DrugBank Data that Cites this Article

Polypeptides

Name	UniProt ID
Glucokinase	P35557	Details

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
3-[(4-fluorophenyl)sulfanyl]-N-(4-methyl-1,3-thiazol-2-yl)-6-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]pyridine-2-carboxamide	Glucokinase	EC 50 (nM)	250	N/A	N/A	Details