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

Abstract:

: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.

journal_name

Medchemcomm

journal_title

MedChemComm

authors

Sokolova AS,Yarovaya OI,Semenova MD,Shtro AA,Orshanskaya IR,Zarubaev VV,Salakhutdinov NF

doi

10.1039/c6md00657d

subject

Has Abstract

pub_date

2017-03-03 00:00:00

pages

960-963

issue

5

eissn

2040-2503

issn

2040-2511

pii

c6md00657d

journal_volume

8

pub_type

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