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 journalArticle

9 Citations (Scopus)

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 languageEnglish (US)
Pages (from-to)531-535
Number of pages5
JournalMedChemComm
Volume2
Issue number6
DOIs
StatePublished - Jun 2011
Externally publishedYes

Fingerprint

Pyrans
Glucokinase
Triazoles
Enantiomers
Amides

ASJC Scopus subject areas

  • Biochemistry
  • Pharmaceutical Science

Cite this

N-(5-substituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl) propanamides as glucokinase activators. / Liu, Zhiqing; Zhu, Qingzhang; Li, Fuying; Zhang, Lina; Leng, Ying; Zhang, Ao.

In: MedChemComm, Vol. 2, No. 6, 06.2011, p. 531-535.

Research output: Contribution to journalArticle

Liu, Zhiqing ; Zhu, Qingzhang ; Li, Fuying ; Zhang, Lina ; Leng, Ying ; Zhang, Ao. / N-(5-substituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl) propanamides as glucokinase activators. In: MedChemComm. 2011 ; Vol. 2, No. 6. pp. 531-535.
@article{c387f97e20c34a768823fb03e6d094ec,
title = "N-(5-substituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl) propanamides as glucokinase activators",
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.",
author = "Zhiqing Liu and Qingzhang Zhu and Fuying Li and Lina Zhang and Ying Leng and Ao Zhang",
year = "2011",
month = "6",
doi = "10.1039/c1md00002k",
language = "English (US)",
volume = "2",
pages = "531--535",
journal = "MedChemComm",
issn = "2040-2503",
publisher = "Royal Society of Chemistry",
number = "6",

}

TY - JOUR

T1 - N-(5-substituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl) propanamides as glucokinase activators

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.

UR - http://www.scopus.com/inward/record.url?scp=79959207838&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=79959207838&partnerID=8YFLogxK

U2 - 10.1039/c1md00002k

DO - 10.1039/c1md00002k

M3 - Article

VL - 2

SP - 531

EP - 535

JO - MedChemComm

JF - MedChemComm

SN - 2040-2503

IS - 6

ER -