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    Please use this identifier to cite or link to this item: http://asiair.asia.edu.tw/ir/handle/310904400/8404


    Title: D-420720, A Novel Orally Active Sulfonamide Compound Dipeptidyl Peptidase IV Inhibitor: Structure and Activity Relationship of Arylsuffonamide to Dipeptidyl Peptidase IV Inhibition
    Authors: Tsai, HJ (Tsai, Henry J.);Chou, SY (Chou, Shan-Yen);Chuang, SH (Chuang, Shih-Hsien);Chen, CC (Chen, Chien-Cheng);Hsu, FL (Hsu, Feng-Lin)
    Contributors: 保健系
    Keywords: dipeptidyl peptidase IV;inhibitor;sulfonamide;diabetes;GLUCAGON-LIKE PEPTIDE-1;IMPROVED GLUCOSE-TOLERANCE;CELL PROLINE DIPEPTIDASE;ANTIHYPERGLYCEMIC PROPERTIES;SERINE-PROTEASE;CD26;PATHWAY;IV/CD26;POTENT;RATS
    Date: 2008-12
    Issue Date: 2010-03-26 10:46:27 (UTC+8)
    Publisher: Asia University
    Abstract: Diabetes mellitus is a chronic disease characteristic of poor glucose homeostasis that requires constant monitoring and adjustment of blood glucose levels by exogenous intervention. Glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) are two incretin peptide hormones secreted from the intestine to synergize insulin's function at lowering blood glucose. The effects of GLP-1 or GIP administration are short-lived because they are rapidly inactivated by circulating dipeptidyl peptidase IV (DPP-IV). Therefore, DPP-IV inhibitors have been suggested to be a new class of molecule for treating hyperglycemic conditions in diabetic patients. The recent approval of Merck's Sitagliptin (a DPP-IV-specific inhibitor) indicates that DPP-IV inhibition is a good target for new therapeutic agent development. The present study was conducted to evaluate the efficacies of a series of dipeptidyl derivatives with a sulfonamide moiety as DPP-IV inhibitors. Among these compounds, D-420720 was a potent inhibitor (K-i = 39 nM), with a selectivity of 9160-fold over the DPP-II isozyme and elicits a hypoglycemic effect on oral glucose tolerance test with normal male ICR mice. Drug Dev Res 69:514-519,2008 (C) 2008 Wiley-Liss, Inc.
    Relation: DRUG DEVELOPMENT RESEARCH, 69(8):514-519.
    Appears in Collections:[食品營養與保健生技學系] 期刊論文

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