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

Zhiqing Liu; Qingzhang Zhu; Fuying Li; Lina Zhang; Ying Leng; Ao Zhang

doi:10.1039/c1md00002k

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

Zhiqing Liu, Qingzhang Zhu, Fuying Li, Lina Zhang, Ying Leng, Ao Zhang

Research output: Contribution to journal › Article › peer-review

11 Scopus citations

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-enantiomer R-15 showed similar potency (0.22 μM) that deserves for further evaluation.

Original language	English (US)
Pages (from-to)	531-535
Number of pages	5
Journal	MedChemComm
Volume	2
Issue number	6
DOIs	https://doi.org/10.1039/c1md00002k
State	Published - Jun 2011
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Pharmacology
Pharmaceutical Science
Drug Discovery
Organic Chemistry

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10.1039/c1md00002k

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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-enantiomer R-15 showed similar potency (0.22 μM) that deserves for further evaluation.",

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AU - Liu, Zhiqing

AU - Zhu, Qingzhang

AU - Li, Fuying

AU - Zhang, Lina

AU - Leng, Ying

AU - Zhang, Ao

PY - 2011/6

Y1 - 2011/6

N2 - 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-enantiomer R-15 showed similar potency (0.22 μM) that deserves for further evaluation.

AB - 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-enantiomer R-15 showed similar potency (0.22 μM) that deserves for further evaluation.

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

Abstract

ASJC Scopus subject areas

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