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標題: Benzene-di-N-octylcarbamates as conformationally constrained phospholipase A(2) inhibitors
作者: Lin, G.
Lin, Y.F.
Hwang, M.T.
Lin, Y.Z.
關鍵字: transition-state analog;cholesterol esterase;elementary processes;protease;complex;acid
Project: Bioorganic & Medicinal Chemistry Letters
期刊/報告no:: Bioorganic & Medicinal Chemistry Letters, Volume 14, Issue 3, Page(s) 751-755.
Conformationally constrained 1,2-, 1,3-, and 1,4- benzene-di-N-octylcarbamates are potent reversible competitive inhibitors of Naja mocambique mocambique phospholipase A(2) with the K-i values of 11, 4, and 15 muM, respectively. With the angle of 1201 between two C(benzene)-O bonds, 1,3-benzene-di-N-octylcarbamate mimics the preferable eclipsed C(sn-2)-O/C(sn-3)-O conformer of phospholipid in the enzyme-phospholipid complex. Further, a three-step phospholipase A(2) inhibition mechanism by the inhibitor is proposed. (C) 2003 Elsevier Ltd. All rights reserved.
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2003.11.047
Appears in Collections:化學系所

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