当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY期刊下所有文献 > Tautomeric and non-tautomeric N-substituted 2-iminobenzimidazolines as new lead compounds for the design of anti-influenza drugs: An in vitro study.

Tautomeric and non-tautomeric N-substituted 2-iminobenzimidazolines as new lead compounds for the design of anti-influenza drugs: An in vitro study.

Abstract：

:A series of 1,3-disubstituted 2-iminobenzimidazolines as well as a number of their tautomeric analogs were synthesized. The synthesized compounds were tested for their cytotoxicity against MDCK cells and for inhibiting activity against influenza virus A/California/07/09 (H1N1)pdm09. Based on the results obtained, 50% cytotoxic concentration (CC50), 50% inhibiting concentration (IC50) and selectivity index (SI) were calculated for each compound. It was found that some of synthesized benzimidazole derivatives (7 of 22, 32%) possess strong virus-inhibiting activity against pandemic influenza virus (IC50's in low micromolar range) with quite moderate cytotoxicity (CC50 in the range of thousands micromoles). Due to their high selectivity (highest SI's=50-83) these compounds are of significant interest for further in vivo experiments as well as for further structural optimization and drug development.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Zarubaev VV,Morkovnik AS,Divaeva LN,Karpinskaya LA,Borodkin GS

doi

10.1016/j.bmc.2016.09.036

subject

Has Abstract

pub_date

2016-11-15 00:00:00

pages

5796-5803

issue

22

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(16)30726-X

journal_volume

24

pub_type

杂志文章

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