12th International Conference of Pharmaceutical Sciences

Organic synthesis promotes the study of new compounds with pharmacological potential. Thus, the present study evaluated the effect of 4-aminoantipyrine (4-AA) and analogues (maleic acid, maleimide, maleimide ester and Diels Alder adduct) on the recruitment of leukocytes to the peritoneal cavity and induction of edema paw, in mice. Male Swiss mice between 18 - 25g (CEUA 949/2018) were used. The experiments were conducted according to Souza and Ferreira (1985; leukocyte recruitment) and Winter et al. (1962; paw edema). The dose used was 48 mg / kg (preliminary trials). Results as mean ± SEM, ANOVA, Bonferroni (p <0.05). Maleimide ester reduced polymorphonuclear recruitment by 61.8% (769.6 ± 308.8 cells / mm3) when compared to the control (2016.0 ± 308.1cel / mm3). The results of paw edema are shown in the following table:

Group Paw edema (mL) and % inhibition
30 min % 60 min % 120 min % 240 min %
Control 0.034±0.004 0.066±0.012 0.040±0.003 0.075±0.007
4-AA 0.028±0.004 17.7 0.052±0.004 21.2 0.042±0.006 5.0 0.046±0.007* 38.7 Maleic acid 0.040±0.00417.7 0.032±0.005* 51.5 0.038±0.006 5.0 0.058±0.009 22.7
Maleimide 0.032±0.004 5.9 0.038±0.004* 42.4 0.036±0.005 10.0 0.046±0.009* 38.7
Maleimide ester 0.046±0.007 35.3 0.045±0.002 31.8 0.037±0.007 7.5 0.082±0.014 9.3
Diels Alder adduct 0.052±0.007 52.9 0.034±0.005* 51.5 0.026±0.002 35.0 0.066±0.009 12.0
Values are expressed as the mean±SEM (n=5). Data were analyzed by two-way ANOVA followed by Bonferroni’s Test for comparisons between groups. *Statistical significance: p<0.05 when compared with the control.

The study contributes to the discovery of the potential of 4-AA and its analogues as a prototype anti-inflammatory drug.