Tautomeric and non-tautomeric N-substituted 2-iminobenzimidazolines as new lead compounds for the design of anti-influenza drugs: An in vitro study |
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| Institution: | 1. Influenza Research Institute, St. Petersburg, Russia;2. Southern Federal University, Rostov-on-Don, Russia;1. Department of Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA;2. Department of Biology, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA;1. LiS Consulting, Lawrence, KS, United States;2. iDDPartners, Princeton Junction, NJ, United States |
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| 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. |
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| Keywords: | 2-Iminobenzimidazolines 2-Acylaminobenzimidazoles 2-Thioureidobenzimidazoles Influenza virus Antiviral activity Cytotoxicity |
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