Searching for new anti-shock substances among 2-phenyliminothiazole derivatives

Abstract

In previous papers we described the synthesis of a new series of derivatives of 2-[4-aryl(adamantyl)- 2-phenyliminothiazol-3-yl]ethanol and described results of in silico studies of pharmacological activity, bioavailability and toxicity of these compounds. Based on results obtained the pharmacological screening for anti-inflammatory activity on the model of histamine edema in mice was studied. As the reference drug claritin was used. It was found that in the majority of substances under research the intensity of the anti-inflammatory activity was dose-dependent. The antihistaminic properties were studied in «Ophthalmic response to introduction of histamine» test in guinea pigs for 3 most active compounds. In this test the activity of 2-[4-(41 -chlorophenyl)-2-phenyliminothiazol-3- yl]-ethanol hydrobromide was statistically significantly higher than that of other compounds and slightly inferior to the reference drug. Results obtained substantiated the feasibility of further studying the anti-shock activity of the most active substance ‒ 2-[4-(41 -chlorophenyl)-2-phenyliminothiazol-3-yl]-ethanol hydrobromide on the model of anaphylactic shock in guinea pigs. It has been found that this compound is somewhat inferior (65%) the action of claritin (78%) by its ability to inhibit development of general anaphylaxis.