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Structure Activity Relationships of 4‐Substituted 1‐Acyl and 1,2‐Diacyl‐1,2,4‐triazolidine‐3,5‐diones as Anti‐inflammatory Agents in Rodents
Author(s) -
Hall Iris H.,
Simlot Rupendra,
Izydore Robert A.
Publication year - 1995
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19953280103
Subject(s) - chemistry , enzyme , pharmacology , acylation , pleurisy , prostaglandin , leukotriene , biochemistry , inflammation , stereochemistry , biology , immunology , medicine , surgery , pleural effusion , asthma , catalysis
Abstract 1‐Acyl and 1,2‐diacyl 1,2,4‐triazolidine‐3,5‐diones proved to be potent anti‐inflammatory agents in rodents at 8 or 20 mg/kg. They were effective against induced edema, pleurisy, and septic shock. Furthermore, these agents were potent in blocking the writhing reflex suggesting that they should be effective against local pain generated by inflammatory processes. These compounds were not lysosomal hydrolytic enzyme or proteolytic enzyme inhibitors in mouse liver, macrophages or human leukocytes. However, the agents were potent inhibitors of prostaglandin and leukotriene de novo synthesis and have potential in acting as free radical scavengers.