Противовоспалительная и анальгезирующая активность производных полиметиленимидазолов

Abstract

The search for new analgesic and anti-inflammatory drugs, exceeding by efficacy and/or safety the existing analogues is very important and relevant. The nitrogenous heterocycles are promising in this respect, in particular, the compounds containing an imidazol moiety. The conducted PASS-prognosis of seven new derivatives of 4.5-polimetilenimidazol has showed a significant probability of their having anti-exudative and anti-nociceptive effects. These effects can be connected both with the influence on the certain links of inflammatory process and with the lack of analgesic effect without an inflammatory component. The toxicity and the specific activity studies have been carried out on the white nonlinear mice. The studied compounds used in a single intragastric administration by the level of toxicity are referred to low or moderate ones. The experimental verification has been carried out on the models of carrageenan edema (anti-exudative action) and “hot plate” (anti-nociceptive action). The substance has been used in a single intragastric administration in a dose of 1/10 LD50. Diclofenac has been used as a reference product in the doses of 3.2 mg/kg (hot plate) and 8 mg/kg (carrageenan edema). The experimental verification has shown a significant validity of the PASS-prognosis and the anti-nociceptive and anti-exudative effects of the derivatives. The most promising compound D-32 has showed a significant anti-exudative activity (-50.0%) and analgesic effect (+110.3%) in the experiment, which is comparable to an active comparator diclofenac: -45.57% and +109.0% respectively.