含有 5-羟基-6-甲基尿嘧啶与 N-乙酰半胱氨酸复合物的制剂的毒性和抗缺氧活性

IF 0.8 4区医学 Q4 CHEMISTRY, MEDICINAL

Pharmaceutical Chemistry Journal Pub Date : 2024-06-22 DOI:10.1007/s11094-024-03131-z

G. G. Kutlugildina, Yu. S. Zimin, A. R. Gimadieva, E. F. Repina, E. R. Kudoyarov

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引用次数: 0

摘要

研究表明，5-羟基-6-甲基尿嘧啶（5-OH-6-MU）与 N-乙酰半胱氨酸（N-AC）形成了 1:1 的复合物，即这两种化合物以等摩尔比相互作用。研究了稳定常数在 291-316 K 范围内的温度依赖性，并确定了络合过程的热力学参数。根据研究结果制定了合成 5-OH-6-MU...N-AC 复合物的程序。随后研究了该复合物的毒性和抗缺氧活性。合成的化合物在小鼠体内的剂量为 500 毫克/千克时，毒性低，抗缺氧活性明显优于参考药物（5-OH-6-MU 和 N-AC）。

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Toxicity and Antihypoxic Activity of a Preparation Containing a Complex Compound of 5-Hydroxy-6-Methyluracil with N-Acetyl Cysteine

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Toxicity and Antihypoxic Activity of a Preparation Containing a Complex Compound of 5-Hydroxy-6-Methyluracil with N-Acetyl Cysteine

5-Hydroxy-6-methyluracil (5-OH-6-MU) was shown to form a 1:1 complex with N-acetylcysteine (N-AC), i.e., the compounds interacted in an equimolar ratio. The temperature dependence of the stability constant was studied in the range 291-316 K. The thermodynamic parameters of the complexation process were determined. Aprocedure for the synthesis of the 5-OH-6-MU…N-AC complex was developed based on the results. The toxicity and antihypoxic activity of the complex were subsequently studied. The synthesized compound at a dose of 500 mg/kg in mice had low toxicity and antihypoxic activity significantly superior to those of the reference drugs (5-OH-6-MU and N-AC).

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来源期刊

Pharmaceutical Chemistry Journal CHEMISTRY, MEDICINAL-PHARMACOLOGY & PHARMACY

CiteScore

1.30

自引率

22.20%

发文量

226

审稿时长

3-8 weeks

期刊介绍： Pharmaceutical Chemistry Journal is a monthly publication devoted to scientific and technical research on the creation of new drugs and the improvement of manufacturing technology of drugs and intermediates. International contributors cover the entire spectrum of new drug research, including: methods of synthesis; results of pharmacological, toxicological, and biochemical studies; investigation of structure - activity relationships in prediction of new compounds; methods and technical facilities used; and problems associated with the development of ecologically safe and economically feasible methods of industrial production. In addition, analytical reviews of the international literature in the field provide coverage of the most recent developments around the world. Pharmaceutical Chemistry Journal is a translation of the Russian journal Khimiko-Farmatsevticheskii Zhurnal. The Russian Volume Year is published in English from April. All articles are peer-reviewed.