New Derivative of Pyrrole and Carnosine: Synthesis, Physicochemical Properties, and Biological Acivity

IF 0.8 4区 医学 Q4 CHEMISTRY, MEDICINAL
T. N. Fedorova, O. I. Kulikova, V. A. Migulin, O. A. Muzychuk, D. A. Abaimov, S. L. Stvolinsky
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Abstract

The new conjugate compound pyrrolylcarnosine was synthesized from the natural antioxidant carnosine and the aromatic five-membered nitrogen heterocycle pyrrole. The synthesis of pyrrolylcarnosine was described. Its physicochemical properties and biological activity in various oxidative stress models were evaluated. The results showed that pyrrolylcarnosine was characterized by resistance to hydrolysis by serum carnosinase and exhibited high antioxidant activity in model experiments. It had a neuroprotective effect under oxidative stress induced by the neurotoxin AAPH, increasing the viability of a differentiated culture of human neuroblastoma SH-SY5Y and protecting it from death. In general, the results indicated creation of a new drug based on pyrrolylcarnosine was promising.

Abstract Image

吡咯和肉碱的新衍生物:合成、理化性质和生物活性
由天然抗氧化剂肌肽和芳香族五元氮杂环吡咯合成了新的共轭化合物吡咯肉碱。对吡咯肉碱的合成进行了描述。对其理化性质和在各种氧化应激模型中的生物活性进行了评估。结果表明,吡咯肉碱具有抗血清肉毒碱酶水解的特点,并在模型实验中表现出较高的抗氧化活性。在神经毒素 AAPH 诱导的氧化应激条件下,它具有神经保护作用,能提高分化培养的人神经母细胞瘤 SH-SY5Y 的存活率,使其免于死亡。总之,研究结果表明,以吡咯烷酮苷为基础开发一种新药是很有希望的。
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来源期刊
Pharmaceutical Chemistry Journal
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.
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