A. V. Shchepochkin, A. F. Uglova, I. A. Utepova, E. S. Gradoblyanskaya, M. A. Averkov, N. V. Kovaleva, E. V. Rudakova, N. P. Boltneva, O. G. Serebryakova, G. F. Makhaeva, V. N. Charushin, O. N. Chupakhin
{"title":"Amino Derivatives of Acridine: Synthesis and Study of Anticholinesterase and Antioxidant Activity","authors":"A. V. Shchepochkin, A. F. Uglova, I. A. Utepova, E. S. Gradoblyanskaya, M. A. Averkov, N. V. Kovaleva, E. V. Rudakova, N. P. Boltneva, O. G. Serebryakova, G. F. Makhaeva, V. N. Charushin, O. N. Chupakhin","doi":"10.1134/S0012500823700167","DOIUrl":null,"url":null,"abstract":"<p>A simple and feasible approach to the synthesis of new amine derivatives of acridine based on the methodology of direct C–H functionalization has been developed. The inhibitory effect of the synthesized compounds toward cholinesterases and carboxylesterase as well as their antioxidant activity have been studied. A high anti-BChE activity has been shown for <i>N</i>-methylpiperazine derivative promising for further optimization to design on its basis new series of compounds efficient for the treatment of neurodegenerative diseases.</p>","PeriodicalId":530,"journal":{"name":"Doklady Chemistry","volume":null,"pages":null},"PeriodicalIF":0.8000,"publicationDate":"2023-06-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Doklady Chemistry","FirstCategoryId":"92","ListUrlMain":"https://link.springer.com/article/10.1134/S0012500823700167","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
引用次数: 0
Abstract
A simple and feasible approach to the synthesis of new amine derivatives of acridine based on the methodology of direct C–H functionalization has been developed. The inhibitory effect of the synthesized compounds toward cholinesterases and carboxylesterase as well as their antioxidant activity have been studied. A high anti-BChE activity has been shown for N-methylpiperazine derivative promising for further optimization to design on its basis new series of compounds efficient for the treatment of neurodegenerative diseases.
期刊介绍:
Doklady Chemistry is a journal that publishes new research in chemistry and chemical engineering of great significance. Initially the journal was a forum of the Russian Academy of Science and published only best contributions from Russia in the form of short articles. Now the journal welcomes submissions from any country in the English or Russian language. Every manuscript must be recommended by Russian or foreign members of the Russian Academy of Sciences.