Assessment of the biological effects of 4-hydrazinoquinoline derivatives

Y. Romanenko, O. Klimova, O. Brazhko
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Abstract

Lipophilicity, biological activity and acute toxicity are important indicators of the viability of drugs. These indicators primarily depend on the chemical structure of the compound, the diversity of functional groups and their quantity. Using ChemDraw, a combinatorial library was created and the lipophilicity and solubility of 4-hydrazinoquinoline oxo acid derivatives were studied. A lipophilic non-polar substance dissolves in the lipid layer of the cell membrane, and the higher the lipophilicity, the greater the ability to penetrate through the cell membrane into substances. In parallel, the solubility of the substances was determined. Virtual studies using PASS Online made it possible to predict biological activity for 4-hydrazinopochid quinoline and their analogues having a methyl group in the 2nd position of azaheterocycles (4-hydrazinoquinaldins). The LD50 value is one of the important characteristics of acute toxicity. The goals of studying acute toxicity are to determine the harmless, toxic, lethal doses of a substance, its ability to cumulate, and also the causes of death of animals. Acute toxicity of lithium (E)-2-(2-(2-methylquinolin-4-yl)hydrazinylidene)pentanedioate was experimentally investigated. The cytotoxic effect of the compounds was tested on cell division and cell growth of cucumber roots (kind «Konkurent»). The study of the growth-regulating activity of lithium (E)-2-(2-(2-methylquinolin-4-yl)hydrazinoylidene)pentanedioate showed that this salt is most active as a cytokine and is classified as a toxicological classification for low toxic substances. Studies on prokaryotes have shown that the pigment-stimulating ability is enhanced in proportion to the concentration of lithium (E)-2-(2-(2-methylquinolin-4-yl)hydrazinoylidene)pentanedioate in nutrient media for individual cultures.
4-肼喹啉衍生物的生物效应评价
亲脂性、生物活性和急性毒性是药物生存力的重要指标。这些指标主要取决于化合物的化学结构、官能团的多样性及其数量。利用ChemDraw建立组合文库,研究了4-肼喹啉氧酸衍生物的亲脂性和溶解度。一种亲脂性非极性物质溶解在细胞膜的脂质层中,亲脂性越高,穿透细胞膜进入物质的能力越大。同时,测定了物质的溶解度。利用PASS Online进行虚拟研究,可以预测4-肼杂环喹啉及其在氮杂环第2位有甲基的类似物(4-肼喹啉)的生物活性。LD50值是急性毒性的重要特征之一。研究急性毒性的目的是确定一种物质的无害、有毒和致死剂量,它的累积能力,以及动物死亡的原因。实验研究了戊二酸锂(E)-2-(2-(2-甲基喹啉-4-基)肼基)的急性毒性。研究了这些化合物对黄瓜根细胞分裂和细胞生长的细胞毒作用。对(E)-2-(2-(2-(2-甲基喹啉-4-基)肼酰亚基)戊二酸锂的生长调节活性的研究表明,该盐作为细胞因子的活性最高,属于低毒物质的毒理学分类。对原核生物的研究表明,在单个培养的营养培养基中,刺激色素的能力与锂(E)-2-(2-(2-甲基喹啉-4-基)肼酰亚基)戊二酸盐的浓度成正比。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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