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DPP-IV inhibitors of the synthesis and activity of

Author: PengMin
Tutor: FangDu
School: Hunan University of Traditional Chinese Medicine
Course: Medicinal Chemistry
Keywords: TypeⅡdiabetes DPP-Ⅳinhibitors Triazole group Anti-diabetic activity
CLC: R914
Type: Master's thesis
Year: 2011
Downloads: 24
Quote: 0
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Abstract


Diabetes can be divided into insulin-dependent (typeⅠ) and non-insulin dependent (typeⅡ), including typeⅡdiabetes is most common, accounting for more than 90% of diabetic patients. Because the pathogenesis of diabetes complicated mankind has yet to find a cure for, which means that patients need lifelong treatment. As the pathophysiology of diabetes-depth understanding of different pathophysiological aspects of drug development is increasing. Dipeptidyl peptidaseⅣinhibitor (dipeptidyl peptidase-4 inhibitor, DPP-Ⅳinhibitors) is currently developing a new, efficient one of hypoglycemic agents. It inhibits the activity of DPP-4 to enhance incretion activity, thereby reducing blood sugar, diabetes; drug therapy has become the new focus. In recent years, several DPP-Ⅳinhibitors have been listed or clinical studies, including MK-0431, NVP-LAF237, BMS-477118, and SYR-322 and so on.βamino acid series of derivatives, as a new class of DPP-Ⅳinhibitors have been extensively studied. Through the synthesis of these compounds and biological activity found in MK-0431, is now available. With independent intellectual property rights for the development of DPP-Ⅳinhibitors,MK-0431 as our lead compound, using a variety of substituted [1,2,3] triazole-based replace the MK-0431 molecule 3-trifluoromethyl [1,2,4] triazole structure. A novel series of MK-0431 analogues (TM1-TM14) were synthesized and evaluated for their in vitro anti- diabetic activity to find new anticancer candidates with more potent activity than MK-0431. The analogues were identified and confirmed by HPLC, 1HNMR and MS.Pharmacological tests showed that, compared with MK-0431, most of the analogues showed strong anti-diabetic activity. Compounds (TM10) were rat pharmacokinetics in vivo glucose tolerance tests and experiments. Shows a strong inhibitory effect of glucose tolerance.

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