Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2024-02-13 , DOI: 10.1007/s00044-024-03191-6 Alexandrina S. Volobueva , Anton A. Shetnev , Mikhail G. Mikhalski , Valeria A. Panova , Darina D. Barkhatova , Ekaterina D. Korshunova , Sergey A. Ivanovskiy , Vladimir V. Zarubaev , Sergey V. Baykov
Indoline-5-sulfonamide derivatives of benzocaine have been synthesized using a sequence of three reactions: N-acylation, sulfochlorination, sulfonamidation, and their antienteroviral activity has been evaluated. Two compounds, namely, ethyl 4-((1-(cyclobutanecarbonyl)indoline)-5-sulfonamido)benzoate and ethyl 4-((1-benzoylindoline)-5-sulfonamido)benzoate exhibited a medium level of activity against coxsackievirus B3 (Nancy strain) in vitro. Their antiviral potential is exerted upon prophylactic application when added to cell culture before infection with the virus.
中文翻译:
苯佐卡因-N-酰基吲哚啉缀合物:合成和针对柯萨奇病毒 B3 的抗病毒活性
使用三个反应序列合成了苯佐卡因的二氢吲哚-5-磺酰胺衍生物:N-酰化、磺氯化、磺酰胺化,并评估了它们的抗肠道病毒活性。两种化合物,即 4-((1-(环丁烷羰基)二氢吲哚)-5-磺酰胺基)苯甲酸乙酯和 4-((1-苯甲酰二氢吲哚)-5-磺酰胺基)苯甲酸乙酯,对柯萨奇病毒 B3 表现出中等水平的活性(Nancy菌株)体外。当在感染病毒之前将其添加到细胞培养物中时,它们的抗病毒潜力可在预防性应用时发挥作用。