Inhibition of human leukocyte elastase by derivatives of N-hydroxysuccinimide. A structure-activity-relationship study

…, MJ Brubaker, MA Stanga, JC Castrisos…

Index: Groutas; Brubaker; Stanga; Castrisos; Crowley; Schatz Journal of Medicinal Chemistry, 1989 , vol. 32, # 7 p. 1607 - 1611

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Citation Number: 70

Abstract

A series of compounds derived from 3-alkyl-N-hydroxysuccinimide have been synthesized and their inhibitory activity toward human leukocyte elastase has been investigated. Compounds having an isobutyl or isopropyl group at the C-3 position have been found to be particularly effective inactivators of the enzyme. The introduction of a trans-styryl group (as in compounds 16 and 18) results in a drastic enhancement in inhibitory activity indicative of ...