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Saint Petersburg, Russia

Sokolova A.S.,Novosibirsk State University | Yarovaya O.I.,Novosibirsk State University | Shernyukov A.V.,RAS Institute of Organic Chemistry | Gatilov Y.V.,Novosibirsk State University | And 6 more authors.
European Journal of Medicinal Chemistry

A new class of compounds featuring a camphor moiety has been discovered that exhibits potent inhibitory activity against influenza A(H1N1)pdm09 and A(H5N1) viruses. The synthesized compounds were characterized by spectroscopic analysis; in addition the structures of compound 2 and 14 were elucidated by the X-ray diffraction technique. Structure-activity relationship studies have been conducted to identify the 1,7,7-trimethylbicyclo[2.2.1]heptanes2-ylidene group as the key functional group responsible for the observed antiviral activity. The most potent antiviral compound is imine 2 with therapeutic index more than 500. © 2015 Elsevier Masson SAS. Source

Zarubaev V.V.,Influenza Research Institute | Garshinina A.V.,Influenza Research Institute | Kalinina N.A.,Influenza Research Institute | Shtro A.A.,Influenza Research Institute | And 4 more authors.

Respiratory viral infections constitute the most frequent reason for medical consultations in the World. They can be associated with a wide range of clinical manifestations ranging from self-limited upper respiratory tract infections to more devastating conditions such as pneumonia. In particular, in serious cases influenza A leads to pneumonia, which is particularly fatal in patients with cardiopulmonary diseases, obesity, young children and the elderly. In the present study, we show a protective effect of the low-molecular weight compound Ingavirin (6-[2-(1H-imidazol-4-yl)ethylamino]-5-oxohexanoic acid) against influenza A (H1N1) virus, human parainfluenza virus and human adenovirus infections in animals. Mortality, weight loss, infectious titer of the virus in tissues and tissue morphology were monitored in the experimental groups of animals. The protective action of Ingavirin was observed as a reduction of infectious titer of the virus in the lung tissue, prolongation of the life of the infected animals, normalization of weight dynamics throughout the course of the disease, lowering of mortality of treated animals compared to a placebo control and normalization of tissue structure. In case of influenza virus infection, the protective activity of Ingavirin was similar to that of the reference compound Tamiflu. Based on the results obtained, Ingavirin should be considered as an important part of anti-viral prophylaxis and therapy. © 2011 by the authors; licensee MDPI, Basel, Switzerland. Source

Marzi A.,National Institute of Allergy and Infectious Diseases | Halfmann P.,Influenza Research Institute | Hill-Batorski L.,Influenza Research Institute | Feldmann F.,National Institute of Allergy and Infectious Diseases | And 6 more authors.

Zaire ebolavirus is the causative agent of the current outbreak of hemorrhagic fever disease in West Africa. Previously, we showed that a whole Ebola virus (EBOV) vaccine based on a replication-defective EBOV (EBOVΔVP30) protects immunized mice and guinea pigs against lethal challenge with rodent-adapted EBOV. Here, we demonstrate that EBOVΔVP30 protects nonhuman primates against lethal infection with EBOV. Although EBOVΔVP30 is replication-incompetent, we additionally inactivated the vaccine with hydrogen peroxide; the chemically inactivated vaccine remained antigenic and protective in nonhuman primates. EBOVΔVP30 thus represents a safe, efficacious, whole-EBOV vaccine candidate that differs from other EBOV vaccine platforms in that it presents all viral proteins and the viral RNA to the host immune system, which might contribute to protective immune responses. © 2015, American Association for the Advancement of Science. All rights reserved. Source

Dura S.N.T.,RAS N. D. Zelinsky Institute of Organic Chemistry | Zarubaev V.V.,Influenza Research Institute | Anfimov P.M.,Influenza Research Institute | Kiselev O.I.,Influenza Research Institute
Antibiotiki i Khimioterapiya

The problem of prophylaxis and therapy of influenza infections remains one of the priority goals for medical science and practical health care. The review includes the discussion of antiviral activity of Deitiforine, a Russian chemotherapeutic. The data on the toxicity and the specific activity spectrum in cell cultures, chicken embryos and laboratory animals are presented. The problem of the influenza viruses resistance to cage compounds and in particular to rimantadine and Deitiforine is also discussed. Source

Ardashov O.V.,RAS Institute of Organic Chemistry | Zarubaev V.V.,Influenza Research Institute | Shtro A.A.,Influenza Research Institute | Korchagina D.V.,RAS Institute of Organic Chemistry | And 3 more authors.
Letters in Drug Design and Discovery

A number of new derivatives of monoterpenoid with a para-menthane framework 3-methyl-6-(prop-1-en-2- yl)cyclohex-3-ene-1,2-diol (-)-3 were synthesized. The antiviral activity of (-)-3 and its derivatives against the pandemic influenza virus A/California/07/09 (H1N1)v was studied in vitro. Compound (-)-3 was found to be active against this virus (selectivity index 7.5); for mononicotinate (+)-6 the selectivity index was 17. The absolute configuration of compound 6 was shown to be critical for its antiviral activity. © 2011 Bentham Science Publishers Ltd. Source

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