☆ 4.7 Article

Design, synthesis and biological evaluation of thiazole- and indole-based derivatives for the treatment of type II diabetes

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2012)

期刊

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

卷 52, 期 -, 页码 70-81

出版社

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER

DOI: 10.1016/j.ejmech.2012.03.006

关键词

Ap2; Thiazole- and indole-based; TNF-alpha; Diet-induced obesity

类别

Chemistry, Medicinal

资金

National Key Technologies RD Program [2012ZX09103-101-033]

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摘要

Present studies have shown that the lipid carrier has a significant role in several aspects of metabolic syndrome in A-FABP/ap2-deficient mice, including type 2 diabetes and atherosclerosis. 38 Thiazole- and indole-based derivatives were synthesized and investigated for their inhibitory effects on the production of LPS-stimulated TNF-alpha. Among them, 12b exhibited an excellent inhibitory efficiency compared to BMS309403 (95% vs. 85%) at the concentration of 10 mu M and a binding affinity for ap2 with the apparent K-i values 33 nM. Oral administration of 12b at a dosage of 50 mg/kg effectively reduced the levels of plasma blood glucose, triglycerides, insulin, total cholesterol and alanine aminotransferase in high-fat/diet-induced obesity model. The results highlighted that 12b was a potent anti-diabetic agent. (C) 2012 Elsevier Masson SAS. All rights reserved.

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