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Company Abstracts :: 1998 :: Selected Company Abstract
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THE STRUCTURE-ACTIVITY
RELATIONSHIPS OF A SERIES OF SUICIDE INHIBITORS OF PHOSPHOLIPASE
A2
Lin Yu, Robert J. Ternansky, Edward J. Victoria, Julia Chang, and
Stephen M. Coutts
La Jolla Pharmaceutical Company, 6455 Nancy Ridge Drive, San Diego,
CA 92121, USA
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.
Published in
Bioorganic & Medicinal Chemistry Letters
1998
Volume 8:pp. 2129-2132
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