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Synthesis of novel bridged dinitrogen heterocycles and their evaluation as potential fragments for the design of biologically active compoundsстатья
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: 5 декабря 2014 г.
- Авторы: Kudryavtsev Konstantin V., Shulga Dmitry A., Chupakhin Vladimir I., Sinauridze Elena I., Ataullakhanov Fazly I., Vatsadze Sergey Z.
- Журнал: Tetrahedron
- Том: 70
- Номер: 43
- Год издания: 2014
- Издательство: Pergamon Press Ltd.
- Местоположение издательства: United Kingdom
- Первая страница: 7854
- Последняя страница: 7864
- DOI: 10.1016/j.tet.2014.09.009
- Аннотация: A library of saturated bridged heterocycles based on 3,6-diazabicyclo[3.2.1]octane-2,4-dione and bispidine scaffolds (mean compound molecular weight is approximately 300 Da) with up to three stereocenters and four diversity points has been synthesized. Synthetic scaffold modifications leading to an increase in molecular complexity were studied. Well-defined stereochemical structures of both compound sets was confirmed by X-ray studies and halogenoaryl substituents were inserted appropriately for the design of novel non-basic serine protease inhibitors. Comprehensive molecular modelling has been performed for all synthesized compounds giving rationales of ligand-enzyme interactions with thrombin and trypsin. Biological testing confirmed moderate inhibitory activity of halogen-substituted saturated diazabicyclic small molecules towards thrombin.
- Добавил в систему: Кудрявцев Константин Викторович