Novel synthetic approach to isoxazole derivatives – promising compounds for biological evaluationтезисы доклада

Дата последнего поиска статьи во внешних источниках: 26 февраля 2018 г.

Работа с тезисами доклада


[1] Novel synthetic approach to isoxazole derivatives – promising compounds for biological evaluation / E. B. Averina, D. A. Vasilenko, T. S. Kuznetzova et al. // 3rd Russian Conference on Medicinal Chemistry, Kazan, Russia, September 28 – October 03, 2017. — Kazan, Russia, 2017. — P. 38–38. Recently we elaborated novel synthetic approaches to functionalized 5-nitroisoxazoles basing on the heterocyclization of electrophilic alkenes under the treatment with tetranitromethane in the presence of triethylamine. Further we have unexpectedly found that heterocyclization of aryl substituted unsaturated ketones under the same conditions results in 4-nitroisoxazole. Employing synthetically available α,β-unsaturated esters the necessary frameworks were introduced in the target heterocycles to provide certain types of bioactivities. Moreover, we elaborated the chemoselective methods of nitro group reduction affording to obtain amino- and hydroxylaminoisoxazoles. The versatility of our synthetic methodology allowed to prepare a library of compounds varying the substituents in the 3- 4- and 5-position of isoxazole core and opened the opportunity to construct the compounds with desired biological activities. We carried out the computer modeling and partially experimental investigations of antiviral, antimitotic, neuroprotective activities and antioxidant properties for isoxazole derivatives and found the perspective series of compounds for further investigations.

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