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Synthesis of water-soluble prodrugs of 5-modified 2ʹ-deoxyuridines and their antibacterial activityстатья
Информация о цитировании статьи получена из
Web of Science,
Scopus
Статья опубликована в журнале из списка Web of Science и/или Scopus
Дата последнего поиска статьи во внешних источниках: 11 марта 2020 г.
- Авторы: Negrya Sergey D., Jasko Maxim V., Solyev Pavel N., Karpenko Inna L., Efremenkova Olga V., Vasilyeva Byazilya F., Sumarukova Irina G., Kochetkov Sergey N., Alexandrova Liudmila A.
- Журнал: Journal of Antibiotics
- Том: 73
- Номер: 4
- Год издания: 2020
- Издательство: Japan Antibiotics Research Association/Nihon Koseibusshitsu Gakujutsu Kyogikai
- Местоположение издательства: Japan
- Первая страница: 236
- Последняя страница: 246
- DOI: 10.1038/s41429-019-0273-x
- Аннотация: Recently we have synthesized a set of pyrimidine nucleoside derivatives bearing extended alkyltriazolylmethyl substituents at position 5 of the nucleic base, and showed their significant activity against Mycobacterium tuberculosis virulent laboratory strain H37Rv as well as drug-resistant MS-115 strain. The presence of a lengthy hydrophobic substituent leads to the reduction of nucleoside water solubility making their antibacterial activity troublesome to study. A series of water-soluble forms of 5-modified 2ʹ-deoxyuridines 4a–c and 8a–c were synthesized. They appeared at least two orders more soluble compared with the parent compounds 1a and 1b. Their half-hydrolysis time was 5–12 h, which can be considered optimal for prodrugs used in clinics. Obtained compounds showed moderate activity (MIC 48–95 µg·ml−1) against some Gram-positive bacteria including resistant strains of Staphylococcus aureus and Mycobacterium smegmatis and were low cytotoxic for human cell lines (CD50 >> 100 µg·ml−1).
- Добавил в систему: Сольев Павел Николаевич