Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators.

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Iino T, Sasaki Y, Bamba M, Mitsuya M, Ohno A, Kamata K, Hosaka H, Maruki H, Futamura M, Yoshimoto R, Ohyama S, Sasaki K, Chiba M, Ohtake N, Nagata Y, Eiki J, Nishimura T

Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators.

Bioorg Med Chem Lett. 2009 Oct 1;19(19):5531-8. doi: 10.1016/j.bmcl.2009.08.064. Epub 2009 Aug 21.

PubMed ID

19726182 [ View in PubMed

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Abstract

We describe design, syntheses and structure-activity relationships of a novel class of 4,6-disubstituted quinazoline glucokinase activators. Prototype quinazoline leads (4 and 5) were designed based on the X-ray analyses of the previous 2-aminobenzamide lead classes. Modifications of the quinazoline leads led to the identification of a potent GK activator (21d).

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
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