Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators.

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

Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1357-60. doi: 10.1016/j.bmcl.2009.01.053. Epub 2009 Jan 21.

PubMed ID

19188063 [ View in PubMed

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Abstract

The identification and structure-activity-relationships (SARs) of novel 2-amino benzamide glucokinase activators are described. Compounds in this series were developed to be potent GK activators, and their binding mode to the GK protein was determined by crystal structure analysis. In vivo pharmacokinetic and acute in vivo efficacy studies of compound 18 are also described.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
2-(methylamino)-N-(4-methyl-1,3-thiazol-2-yl)-5-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]benzamide	Glucokinase	EC 50 (nM)	1100	N/A	N/A	Details
2-(methylamino)-N-(4-methyl-1,3-thiazol-2-yl)-5-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]benzamide	Glucokinase	EC 50 (nM)	330	N/A	N/A	Details
2-amino-N-(4-methyl-1,3-thiazol-2-yl)-5-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]benzamide	Glucokinase	EC 50 (nM)	420	N/A	N/A	Details
2-amino-N-(4-methyl-1,3-thiazol-2-yl)-5-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]benzamide	Glucokinase	EC 50 (nM)	140	N/A	N/A	Details