Abstract
The acute toxicity of 17 new derivatives of benzilic acid in outbred mice weighing 20-26 g has been determined. Animals were divided into 68 groups of 5 mice each. Each group of animals received the aqueous solution of the substance under study once orally by gavage in the doses of 100, 250, 750, 1000 mg/kg. The total duration of follow-up of the animals after administration of the test substance was 14 days. Administration of substances under the codes of KMS-10, KMS-19, KMS-49, KMS-68, KMS-70, KMS-71, KMS-73, KMS-228, KMS-230, KMS-284 in the dose of 1000 mg/kg caused no deaths of mice. It suggests that these substances are non-toxic in the selected doses. Since the dose of 1000 mg/kg did not result in the death of animals in these groups, the conclusion can be made that LD50>1000 mg/kg. According to the classification of K.K. Sidorov the substances under study can be referred to Class IV toxicity (low-toxic compounds).
Highlights
Modern drugs should be characterized by low toxicity and high efficiency [4]
The results obtained within 14 days of observation of the laboratory animals received the test compounds in the dose of 1000 mg/kg are given in Tab. 1
On the third and eighth days of the study one animal died from each group receiving the aqueous solutions of products of cyclization of benzilic acid amides containing the fragment of 2-oxo-3,3-diphenyl-2,3-dihydro-1H-thieno[3, 4-b]pyrrole-6-carboxylic acid – KMS-72 and KMS-69, respectively
Summary
Determination of the acute toxicity of substances is the first stage when considering toxicological characteristics; its aim is to obtain information concerning the substance danger to health in terms of the short-term action. These data can be taken as a basis for toxicity class determination. To study the toxicity of substances the pharmacological model, which makes possible to study the effects on the experimental animals, is created. The aim of this study was to determine the acute toxicity of new pharmacologically active derivatives of benzilic acid
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