Вид документа : Статья из журнала Шифр издания : 54/A 37 Автор(ы) : Boltneva N. P., Makhaeva G. F., Kovaleva N. V., Lushchekina S. V., Burgart Ya. V., Shchegol’kov E. V., Chupakhin O. N. Заглавие : Alkyl 2-arylhydrazinylidene-3-oxo-3-polyfluoroalkylpropionates as new effective and selective inhibitors of carboxylesterase [Электронный ресурс] Место публикации : Doklady Biochemistry and Biophysics . - 2015. - Vol. 465, № 1. - С. 381-385 Систем. требования: http://link.springer.com/article/10.1134/S1607672915060101 Примечания : Bibliogr. : p. 385 (15 ref.). - 19.01.2016 ББК : 54 Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ Ключевые слова (''Своб.индексиров.''): 2-arylhydrazinylidene-3-oxo-3-polyfluoroalkylpropionates--inhibitors--carboxylesterase Аннотация: A series of alkyl 2-Arylhydrazinylidene-3-oxo-3-polyfluoroalkylpropionates was synthesized and their inhibitory activity with respect to porcine liver carboxylesterase (CaE, EC 3.1.1.1), human erythrocyte acetylcholinesterase (AChE, EC 3.1.1.7), and horse serum butyrylcholinesterase (BChE, EC 3.1.1.8) was studied. The molecular docking method was used to study the binding mode of the compounds in the active site of CaE. It was found that compounds containing the trifluoromethyl group in the third position of carbonyl chain are highly effective and selective inhibitors of CaE with nanomolar IC50 values, which agrees well with the results of molecular docking. Origin Доп.точки доступа: Boltneva, N. P.; Makhaeva, G. F.; Kovaleva, N. V.; Lushchekina, S. V.; Burgart, Ya. V.; Бургарт Янина Валерьевна; Shchegol’kov, E. V.; Chupakhin, O. N.