新型含噻吩的1,2,4-三唑衍生物的急性毒性研究

IF 0.1 Q4 MEDICINE, GENERAL & INTERNAL
A. Khilkovets, I. Bilai
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引用次数: 1

摘要

急性毒性研究是任何新的生物活性化合物临床前研究的一个组成部分。应该指出的是,这一阶段的研究对于进一步使用药理学活性物质作为药物的可能性至关重要。该指标还有助于确定临床试验的初始剂量,并确定可能安全的剂量范围。所获得的数据将有助于确定新化学合成的方向,补充相关的计算机文库,以及揭示表征化合物-生物系统相互作用的许多其他基本重要参数。本研究的目的是研究2-((4-苯基-5-(噻吩-3-甲基)-1,2,4-三唑-3-基)硫代)乙酸钠的急性毒性。材料和方法。以前,使用GUSAR计算机程序进行了预测,这有助于确定剂量间隔。采用Kerber实验法测定其在体急性毒性,实验对象为白色非线性Wistar大鼠。这些大鼠称重,贴上标签,并分为五组,每组6只。引入复合运动活性降低后,观察到嗜睡、瞳孔缩小和口渴。在第五组,在最大稀释下,所有大鼠在给药后两小时内死亡。在死亡过程中,观察到抽搐。第四组有五只老鼠死亡,第三组有两只老鼠死亡。在前两组中,所有的老鼠都存活了下来。在随访期间,这些动物表现正常。根据研究结果进行了计算,确定了LD50指标。结果表明,所研究化合物属V类毒性(几乎无毒),LD50值为1125 mg/kg。这一指标证实了该化合物进一步研究的前景。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Study of acute toxicity of new thiophene-containing derivatives of 1,2,4-triazole
Acute toxicity studies are an integral part of preclinical studies of any new biologically active compound. It should be noted that it is this stage of research that is crucial regarding the possibility of further use of a pharmacologically active substance as a drug. This indicator also helps to determine the initial dose for clinical trials and establish a range of potentially safe doses. The data obtained will help determine the direction of new chemical syntheses, replenish the relevant libraries in silico, as well as reveal many other fundamentally important parameters that characterize the interaction in the compound – living organism system. The aim of this research is to study the acute toxicity of 2-((4-phenyl-5-(thiophene-3-ylmethyl)-1,2,4-triazole-3-yl)thio)sodium acetate. Materials and methods. Previously, a prediction was made using the GUSAR computer program, which helped determine the dose intervals. Acute toxicity was determined by the experimental method of Kerber in vivo using white nonlinear Wistar rats. The rats were weighed, labeled, and divided into five groups of six individuals of each. Results. After the introduction of compound moving activity decreased, drowsiness, pupil miosis, and thirst were observed. In the fifth group, with the maximum dilution, all rats died within two hours after administration of the test compound. During the death, convulsions were observed. In the fourth group five animals died, and in the third – two rats died. In the first two groups, all the rats survived. During follow-up, the animals behaved normally. Based on the results of the research, calculations were made and the LD50 indicator was determined. Conclusions. According to the results, the studied compound belonged to the V class of toxicity (almost non-toxic), and the resulting LD50 value was 1125 mg/kg. This indicator confirmed the prospects for further study of this compound.
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来源期刊
Zaporozhye Medical Journal
Zaporozhye Medical Journal MEDICINE, GENERAL & INTERNAL-
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审稿时长
8 weeks
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