Репозиторий Университета

Год публикации: Все года 2018 2019 2020

Название	Дата публикации	Коллектив авторов	Журнал	DOI	Индекс цитирования	Ссылка на источник
3′-O-Substituted 5-(perylen-3-ylethynyl)-2′-deoxyuridines as tick-borne encephalitis virus reproduction inhibitors Antiviralactivity Cycloaddition Lipophilicity Nucleoside Tick-borneencephalitisvirus	15.07.2018	Proskurin G. Orlov A. Brylev V. Kozlovskaya L. Chistov A. Karganova G. Palyulin V. Osolodkin D. Korshun V. Aralov A.	European Journal of Medicinal Chemistry		5	Ссылка © 2018 Elsevier Masson SAS A series of analogues of potent antiviral perylene nucleoside dUY11 with methylthiomethyl (MTM), azidomethyl (AZM) and HO-C1–4-alkyl-1,2,3-triazol-1,4-diyl groups at 3′-O-position as well as the two products of copper-free alkyne-azide cycloaddition of the AZM derivative were prepared and evaluated against tick-borne encephalitis virus (TBEV). Four compounds (4, 6, 8a, 8b) showed EC50 ≤ 10 nM, thus appearing the most potent TBEV inhibitors to date. Moreover, these nucleosides have higher lipophilicity (clogP) and increased solubility in aq. DMSO vs. parent compound dUY11. Читать тезис
Synthesis and structure—activity relationships of cyclopropane-containing analogs of pharmacologically active compounds cycloaddition cyclopropanes heterocyclization pyrimidines	01.03.2018	Novakov I. Babushkin A. Yablokov A. Nawrozkĳ M. Vostrikova O. Shejkin D. Mkrtchyan A. Balakin K.	Russian Chemical Bulletin		3	Ссылка © 2018, Springer Science+Business Media, LLC, part of Springer Nature. The review summarizes information on cyclopropane as an independent pharmacophore group and as a fragment for modification of pharmacological activity level of medicines used in practice. The advantages of a cyclopropane fragment over its bioisosteres are that, on the one hand, this fragment imposes conformational rigidity on the molecules of physiologically active compounds and, on the other hand, the replacement of acyclic terminal and “linker” groups with a cyclopropane fragment increases the metabolic stability of the target structures and extends the scope of their therapeutic action. Читать тезис

Репозиторий Университета

Перейти в раздел: