Design, Synthesis and Anti-diabetic Activities of Thiazole-Bearing Compounds as Dipeptidyl Peptidase IV Inhibitors

Chin. J. Org. Chem. ›› 2009, Vol. 29 ›› Issue (08): 1236-1242. Previous Articles Next Articles

Original Articles

含噻唑环的二肽基肽酶IV抑制剂的设计、合成和降血糖活性研究

战付旭^a ; 王玉丽^b; 赵桂龙^*,b; 徐为人^b; 李祎亮^b;
邹美香^b; 汤立达^c ; 王建武^*,a

(a山东大学化学与化工学院济南 250100)
(b天津药物研究院分子设计与药物发现天津市重点实验室天津 300193)
(c天津药物研究院药代动力学与药效学省部共建国家重点实验室天津 300193)

收稿日期:2009-01-18 修回日期:2009-02-26 发布日期:2009-08-30
通讯作者: 赵桂龙;王建武

Design, Synthesis and Anti-diabetic Activities of Thiazole-Bearing Compounds as Dipeptidyl Peptidase IV Inhibitors

Zhan, Fuxu^a; Wang, Yuli ^b ;Zhao, Guilong^*,b; Xu, Weiren^b; Li, Yiliang ^b;Zou, Meixiang^b; Tang, Lida^c ; Wang, Jianwu^*,a

(a School of Chemistry and Chemical Engineering, Shandong University, Jinan 250100) (b Tianjin Key Laboratory of Molecular Design and Drug Discovery, Tianjin Institute of Pharmaceutical Research, Tianjin 300193)
(c Tianjintate Key Laboratory of Pharmacokinetics and Phmarcodynamics, Tianjin Institute of Pharmaceutical
Research, Tianjin 300193)

Received:2009-01-18 Revised:2009-02-26 Published:2009-08-30
Contact: Zhao, Guilong; Wang, Jianwu

Abstract

Sixteen thiazole-bearing compounds were designed and synthesized as dipeptidyl peptidase IV (DPP-IV) inhibitors, and characterized by IR, 1H NMR, 13C NMR and HR-MS techniques. Their activities to decrease blood glucose level were determined through a rat oral glucose tolerance test (OGTT) and the result showed that two compounds exhibited potent activities to decrease the blood glucose level, with one being compara-ble with and the other being more potent than gliclazide, which indicates that these two compounds are promising for the treatment of type II diabetes. Careful examination led to the establishment of a regular structure-activity relationship (SAR).

Key words: dipeptidyl peptidase IV, synthesis, oral glucose tolerance test, diabetes, structure-activity relationship, thiazole

Cite this article

Zhan, Fuxu^a; Wang, Yuli ^b ;Zhao, Guilong^*,b; Xu, Weiren^b; Li, Yiliang ^b;Zou, Meixiang^b; Tang, Lida^c ; Wang, Jianwu^*,a
. Design, Synthesis and Anti-diabetic Activities of Thiazole-Bearing Compounds as Dipeptidyl Peptidase IV Inhibitors[J]. Chin. J. Org. Chem., 2009, 29(08): 1236-1242.

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含噻唑环的二肽基肽酶IV抑制剂的设计、合成和降血糖活性研究

Design, Synthesis and Anti-diabetic Activities of Thiazole-Bearing Compounds as Dipeptidyl Peptidase IV Inhibitors

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