Synthesis and in vitro study of novel borneol derivatives as potent inhibitors of the influenza A virus

A. S. Sokolova, O. I. Yarovaya, M. D. Semenova, A. A. Shtro, I. R. Orshanskaya, V. V. Zarubaev, N. F. Salakhutdinov

Результат исследования: Научные публикации в периодических изданияхстатья

15 Цитирования (Scopus)

Аннотация

Herein, we present the design and synthesis of a series of novel heterocyclic derivatives of (-)-borneol and (-)-isoborneol as potent inhibitors of the influenza A virus. All compounds were tested for their toxicity against MDCK cells and for virus-inhibiting activity against the influenza virus A/Puerto Rico/8/34 (H1N1). Compounds 7, 16 and 26 containing a morpholine fragment exhibited the highest efficiency as agents inhibiting the replication of the influenza virus A(H1N1) with selectivity indices of 82, 45 and 65, correspondingly. Derivatives 9 (SI = 23) and 18 (SI = 25) containing a 1-methylpiperazine motif showed moderate antiviral activity. Structure-activity analysis of this new series of borneol derivatives revealed that a 1,7,7-trimethylbicyclo[2.2.1]heptan scaffold is required for the antiviral activity.

Язык оригиналаанглийский
Страницы (с-по)960-963
Число страниц4
ЖурналMedChemComm
Том8
Номер выпуска5
DOI
СостояниеОпубликовано - 1 мая 2017

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