Вид документа : Статья из журнала Шифр издания : 54/S 98 Автор(ы) : Kravchenko M. A., Verbitskiy E. V., Medvinskiy I. D., Rusinov G. L., Charushin V. N. Заглавие : Synthesis and antituberculosis activity of novel 5-styryl-4-(hetero)aryl-pyrimidines via combination of the Pd-catalyzed Suzuki cross-coupling and SNH reactions [Электронный ресурс] Место публикации : Bioorganic and Medicinal Chemistry Letters. - 2014. - Vol. 24, №14. - С. 3118-3120 Систем. требования: http://www.sciencedirect.com/science/article/pii/S0960894X14004934 Примечания : 08.08.2014 ББК : 54 Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ Ключевые слова (''Своб.индексиров.''): pyrimidine--antimicobacterial--tuberculosis Аннотация: Combination of the Suzuki cross-coupling and nucleophilic aromatic substitution of hydrogen (SNH) reactions proved to be a convenient method for the synthesis of 5-styryl-4-(hetero)aryl substituted pyrimidines from commercially available 5-bromopyrimidine. All intermediate 5-bromo-4-(hetero)aryl substituted pyrimidines and also the targeted 5-styryl-4-(hetero)arylpyrimidines were found to be active in micromolar concentrations in vitro against Mycobacterium tuberculosis H37Rv, avium, terrae, and multi-drug-resistant strain isolated from tuberculosis patients in Ural region (Russia). It has been found that some of these compounds possess a low toxicity and have a bacteriostatic effect, comparable and even higher with that of first-line antituberculosis drugs Доп.точки доступа: Kravchenko, M. A.; Verbitskiy, E. V.; Medvinskiy, I. D.; Rusinov, G. L.; Русинов Геннадий Леонидович; Charushin, V. N. |