tetano
Editor, Senior Moderator
Bioorg Med Chem. 2016 Sep 15. pii: S0968-0896(16)30726-X. doi: 10.1016/j.bmc.2016.09.036. [Epub ahead of print]
[h=1]Tautomeric and non-tautomeric N-substituted 2-iminobenzimidazolines as new lead compounds for the design of anti-influenza drugs: An in vitro study.[/h] Zarubaev VV[SUP]1[/SUP], Morkovnik AS[SUP]2[/SUP], Divaeva LN[SUP]2[/SUP], Karpinskaya LA[SUP]3[/SUP], Borodkin GS[SUP]2[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] 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 (CC[SUB]50[/SUB]), 50% inhibiting concentration (IC[SUB]50[/SUB]) 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 (IC[SUB]50[/SUB]'s in low micromolar range) with quite moderate cytotoxicity (CC[SUB]50[/SUB] 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.
Copyright ? 2016 Elsevier Ltd. All rights reserved.
[h=4]KEYWORDS:[/h] 2-Acylaminobenzimidazoles; 2-Iminobenzimidazolines; 2-Thioureidobenzimidazoles; Antiviral activity; Cytotoxicity; Influenza virus
PMID: 27670100 DOI: 10.1016/j.bmc.2016.09.036
[PubMed - as supplied by publisher]
[h=1]Tautomeric and non-tautomeric N-substituted 2-iminobenzimidazolines as new lead compounds for the design of anti-influenza drugs: An in vitro study.[/h] Zarubaev VV[SUP]1[/SUP], Morkovnik AS[SUP]2[/SUP], Divaeva LN[SUP]2[/SUP], Karpinskaya LA[SUP]3[/SUP], Borodkin GS[SUP]2[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] 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 (CC[SUB]50[/SUB]), 50% inhibiting concentration (IC[SUB]50[/SUB]) 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 (IC[SUB]50[/SUB]'s in low micromolar range) with quite moderate cytotoxicity (CC[SUB]50[/SUB] 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.
Copyright ? 2016 Elsevier Ltd. All rights reserved.
[h=4]KEYWORDS:[/h] 2-Acylaminobenzimidazoles; 2-Iminobenzimidazolines; 2-Thioureidobenzimidazoles; Antiviral activity; Cytotoxicity; Influenza virus
PMID: 27670100 DOI: 10.1016/j.bmc.2016.09.036
[PubMed - as supplied by publisher]