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Title: Tautomeric and non-tautomeric N-substituted 2-iminobenzimidazolines as new lead compounds for the design of anti-influenza drugs: An in vitro study
Authors: Morkovnik, Anatolii S
Divaeva, Liudmila N
Karpinskaya, Liubov' A
Borodkin, Gennadii S
Zarubaev, Vladimir V. 
Keywords: 2-Acylaminobenzimidazoles;2-Iminobenzimidazolines;2-Thioureidobenzimidazoles;Antiviral activity;Cytotoxicity;Influenza virus
Issue Date: 2016
Publisher: Elsevier
Journal: Bioorganic and Medicinal Chemistry 
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.
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2016.09.036
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