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Sglt - 2 Diabetes Drug Design And Synthesis Of Inhibitors

Posted on:2014-01-27Degree:MasterType:Thesis
Country:ChinaCandidate:Q X YangFull Text:PDF
GTID:2244330395991513Subject:Medicinal chemistry
Abstract/Summary:PDF Full Text Request
Diabetes can be divided into insulin-dependent (type I) and non-insulin dependent (type II), including type II diabetes is most common, accounting for more than90%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. sodium-glucose co-transporter is currently developing a new, efficient one of hypoglycemic agents. It inhibits the activity of SGLT-2to enhance incretion activity, thereby reducing blood sugar, diabetes; drug therapy has become the new focus. In recent years, several SGLT-2inhibitors have been listed or clinical studies, including Dapagliflozin, Canagliflozin, LX4211,Taisho,TS-071and so on.SGLT-2series of derivatives, as a new class of sodium-glucose co-transporter inhibitors have been extensively studied. With independent intellectual property rights for the development of SGLT-2inhibitors, Dapagliflozin as our lead compound, getting a variety of the analogues of Dapagliflozin. A novel series of Dapagliflozin analogues (1-11) were synthesized and evaluated for their in vitro anti-diabetic activity to find new anticancer candidates with more potent activity than Dapagliflozin. The analogues were identified and confirmed by HPLC,1HNMR and MS.
Keywords/Search Tags:Type â…¡ diabetes, SGLT-2Inhibitors, Dapagliflozin, Anti-diabetic activity
PDF Full Text Request
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