Citation

Yu L, Ternansky RJ, Victoria EJ, Chang J, Coutts SM. Bioorg. Med. Chem. Lett. 1998; 8(16): 2129-2132.

Copyright

(Copyright © 1998, Elsevier Publishing)

DOI

10.1016/s0960-894x(98)00378-3

PMID

9873499

Abstract

A series of mechanism-based inhibitors of phospholipase A2 (SIBLINKS) were synthesized. These new SIBLINKS are phospholipid analogues that contain a para-substituted phenyl 3,3-dimethylglutaryl group in the place of the sn-2 acyl chain. The effect of the phenyl leaving group on inhibitory activity was studied by varying the electron-withdrawing ability of the para-substituted group. A strong correlation was observed between the leaving group potential of the suicide inhibitor and the inhibitory activity of the derivative toward cobra venom phospholipase A2.

Language: en

Keywords

Animals; Drug Design; Elapid Venoms; Elapidae; Enzyme Inhibitors; Kinetics; Molecular Structure; Phenols; Phospholipases A; Phospholipases A2; Phospholipids; Structure-Activity Relationship