M. Dibraccio et al., 1,8-NAPHTHYRIDINES .2. 2,4-DISUBSTITUTED N,N-DIALKYL-1,8-NAPHTHYRIDINE 3-CARBOXAMIDES WITH ANTIINFLAMMATORY AND OR ANTIAGGRESSIVE ACTIVITIES/, Il Farmaco, 49(1), 1994, pp. 25-32
The preparation of the novel lkyl-2,4-dichloro-1,8-naphthyridine-3-car
boxamides 1c,e and N,N-dialkyl-2-(alkylamino or ylamino)-4-chloro-1,8-
naphthyridine-3-carboxamides 2b,d-g,j-p is described. These compounds
and the previously obtained analogs 1a,b,d,f and 2a,c,h,i have been te
sted for their anti-inflammatory and antiaggressive activities, as wel
l as for their gross behavioral effects and acute toxicity. Nine of th
e twenty-two tested compounds exhibited a statistically significant an
ti-inflammatory activity in the carrageenin-induced edema assay in the
rat (1e,f and 2h,o were the most active compounds). On the other hand
, an interesting antiaggressive activity was displayed by ten compound
s in the isolation-induced aggressiveness test in mice (compounds 2d,i
,k showed the highest activity). Structure-activity relationships are
briefly discussed.