1,8-Naphthyridines IV. 9-substituted N,N-dialkyl-5-(alkylamino or cycloalkylamino) [1,2,4]triazolo[4,3-a][1, 8]naphthyridine-6-carboxamides, new compounds with anti-aggressive and potent anti-inflammatory activities.

Abstract:

: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 anti-aggressive 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.

journal_name

Eur J Med Chem

authors

Roma G,Di Braccio M,Grossi G,Mattioli F,Ghia M

doi

10.1016/s0223-5234(00)01175-2

subject

Has Abstract

pub_date

2000-11-01 00:00:00

pages

1021-35

issue

11

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(00)01175-2

journal_volume

35

pub_type

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