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Issue 6, 2011
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N-(5-substituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl) propanamides as glucokinase activators

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Abstract

A series of novel arylacetamides were designed to further explore the GK binding property at the aminothiazole C5 position. The C5-amide substituted aminothiazoles 7a–f generally displayed decreased potency, whereas most of the C5-triazole substituted aminothiazoles retained good GK potency. Triazole 15 with a hydroxyethyl side chain was the most potent among the current series possessing an EC50 value of 0.18 μM. Its R-enantiomerR-15 showed similar potency (0.22 μM) that deserves for further evaluation.

Graphical abstract: N-(5-substituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl) propanamides as glucokinase activators

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Publication details

The article was received on 05 Jan 2011, accepted on 22 Mar 2011 and first published on 14 Apr 2011


Article type: Concise Article
DOI: 10.1039/C1MD00002K
Med. Chem. Commun., 2011,2, 531-535

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    N-(5-substituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl) propanamides as glucokinase activators

    Z. Liu, Q. Zhu, F. Li, L. Zhang, Y. Leng and A. Zhang, Med. Chem. Commun., 2011, 2, 531
    DOI: 10.1039/C1MD00002K

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