Tweet
Eur J Med Chem. 2016 Oct 19. pii: S0223-5234(16)30897-2. doi: 10.1016/j.ejmech.2016.10.035. [Epub ahead of print]
Aliphatic and alicyclic camphor imines as effective inhibitors of influenza virus H1N1.
Sokolova AS1, Yarovaya ОI2, Baev DS3, Shernyukov АV3, Shtro AA4, Zarubaev VV5, Salakhutdinov NF1.
Author information
Abstract
A series of camphor derived imines was synthesised and evaluated in vitro for antiviral activity. Theoretical evaluations of ADME properties were also carried out. Most of these compounds exhibited significant activity against the drug-resistant strains of influenza A virus. Especially, compounds 2 (SI = 632) and 3 (SI = 417) presented high inhibition against influenza subtypes A/Puerto Rico/8/34 and A/California/07/09 of H1N1pdm09. Analysis of the structure-activity relationship showed that the activity was strongly dependent on the length of the aliphatic chain: derivatives with a shorter chain possessed higher activity, while the suppressing action of compounds with long aliphatic chains was lower.
Copyright ? 2016 Elsevier Masson SAS. All rights reserved.
KEYWORDS:
Antiviral; Cage compounds; Camphor derivatives; Influenza
PMID: 27823881 DOI: 10.1016/j.ejmech.2016.10.035
[PubMed - as supplied by publisher]
Aliphatic and alicyclic camphor imines as effective inhibitors of influenza virus H1N1.
Sokolova AS1, Yarovaya ОI2, Baev DS3, Shernyukov АV3, Shtro AA4, Zarubaev VV5, Salakhutdinov NF1.
Author information
Abstract
A series of camphor derived imines was synthesised and evaluated in vitro for antiviral activity. Theoretical evaluations of ADME properties were also carried out. Most of these compounds exhibited significant activity against the drug-resistant strains of influenza A virus. Especially, compounds 2 (SI = 632) and 3 (SI = 417) presented high inhibition against influenza subtypes A/Puerto Rico/8/34 and A/California/07/09 of H1N1pdm09. Analysis of the structure-activity relationship showed that the activity was strongly dependent on the length of the aliphatic chain: derivatives with a shorter chain possessed higher activity, while the suppressing action of compounds with long aliphatic chains was lower.
Copyright ? 2016 Elsevier Masson SAS. All rights reserved.
KEYWORDS:
Antiviral; Cage compounds; Camphor derivatives; Influenza
PMID: 27823881 DOI: 10.1016/j.ejmech.2016.10.035
[PubMed - as supplied by publisher]