THE STRUCTURE-ACTIVITY-RELATIONSHIPS OF A SERIES OF SUICIDE INHIBITORS OF PHOSPHOLIPASE A(2)

Authors
YU L TERNANSKY RJ VICTORIA EJ CHANG J COUTTS SM
Citation
L. Yu et al., THE STRUCTURE-ACTIVITY-RELATIONSHIPS OF A SERIES OF SUICIDE INHIBITORS OF PHOSPHOLIPASE A(2), Bioorganic & medicinal chemistry letters, 8(16), 1998, pp. 2129-2132
Citations number
15
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
16
Year of publication
1998
Pages
2129 - 2132
Database
ISI
SICI code
0960-894X(1998)8:16<2129:TSOASO>2.0.ZU;2-I
Abstract
A series of mechanism-based inhibitors of phospholipase A(2) (SIBLINKS ) were synthesized. These new SIBLINKS are phospholipid analogues that contain a para-substituted phenyl 3,3-dimethylglutaryl group in the p lace of the sn-2 acyl chain. The effect of the phenyl leaving group on inhibitory activity was studied by varying the electron-withdrawing a bility of the para-substituted group. A strong correlation was observe d between the leaving group potential of the suicide inhibitor and the inhibitory activity of the derivative toward cobra venom phospholipas e A(2). (C) 1998 Elsevier Science Ltd. All rights reserved.