Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 35, Issue 11, Pages 1021-1035Publisher
EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/S0223-5234(00)01175-2
Keywords
[1,2,4]triazolo[4,3-a][1,8]naphthyridine derivatives; anti-inflammatory activity; anti-aggressive activity; structure-activity relationships
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The title compounds (8) were synthesized through the cyclocondensation of the corresponding N-substituted 4-amino-2-chloro-1,8-naphthyridine-3-carboxamides (4) with the proper hydrazides, in order to evaluate their anti-inflammatory and antiaggressive properties. Several compounds 8 exhibited high anti-inflammatory activity (carrageenin-induced paw edema assay in the rat) along with appreciable anti-aggressive properties (isolation-induced aggressiveness test in mice). With respect to anti-inflammatory activity, the most active compounds (8n and 8c) produced a 61% edema inhibition at the 25 mg/kg dose, and 50 or 35% inhibition, respectively, at the 12.5 mg/kg dose. The structure-activity relationships are discussed. (C) 2000 Editions scientifiques et medicales Elsevier SAS.
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