Citation

Roma G, Di Braccio M, Grossi G, Mattioli F, Ghia M. Eur. J. Med. Chem. 2000; 35(11): 1021-1035.

Affiliation

Dipartimento di Scienze Farmaceutiche, Università di Genova, Viale Benedetto XV 3, 16132, Genoa, Italy. roma@unige.it

Copyright

(Copyright © 2000, Elsevier Publishing)

DOI

unavailable

PMID

11137230

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.

Language: en