Analgesic and anti-inflammatory activity of 5,7-diacyl-3-H(alkіl)-6- aryl-5H-[1,2,4]triazol[3,4-b][1,3,4]tіadiazin derivaties

Abstract

The search for new analgesic and anti-inflammatory drugs, exceeding by efficacy and/or safety the existing<br />analogues is very important and relevant. The nitrogenous heterocycles are promising in this respect, in particular,<br />the compounds containing an imidazole triazol and tіadiazin moiety. The aim of the current study was to investigate<br />the antiexudative and antinociceptive activity of new derivatives of 5,7-diacyl-3-H(alkyl)-6-aryl-5H[1,2,4]triazol[3,4-b]<br />[1,3,4]thiadiazine.<br />The antinociceptive and antiexudative activity studies were carried out on the white nonlinear mice. The<br />experimental evaluation of specific activity was carried out on the models “Hot plate”, acetic acid induced writhing<br />(antinociceptive action) and carrageenan edema (antiexudative action). The substance was used in a single oral rout<br />administration in a dose of 25 mg/kg. Ketorolac was used as a reference product in the dose of 25 mg/kg (models<br />“Hot plate”, acetic acid induced writhing). Diclofenac was used as a reference product in the dose of 25 mg/kg on<br />the model carrageenan edema. The experimental study showed the antinociceptive and antiexudative effects of the<br />derivatives. The antinociceptive activity of 5,7-diacyl-3-H(alkіl)-6-aryl-5H[1,2,4]triazol[3,4-b][1,3,4]tіadiazin derivaties<br />related to the modification structure in the para position of benzene ring. The antiexudative activity is associated with<br />acetyl groups thiadiazine ring. The most promising compound IFT_247 showed a significant antinociceptive effect,<br />which is comparable to an active comparator ketorolac: “Hot plate” +232.46 % and +112.71 %; acetic acid induced<br />writhing -66.67 % and -61.02 %, respectively.