Recent Studies from Vertex Pharmaceuticals Inc. Add New Data to Antiinfectives (Novel 2-Substituted 7-Azaindole and 7-Azaindazole Analogues as Potential Antiviral Agents for the Treatment of Influenza)
By a News Reporter-Staff News Editor at Biotech Week -- Current study results on Drugs and Therapies - Antiinfectives have been published. According to news originating from Boston, Massachusetts, by NewsRx correspondents, research stated, "JNJ-63623872 (2) is a first-in-class, orally bioavailable compound that offers significant potential for the treatment of pandemic and seasonal influenza. Early lead optimization efforts in our 7-azaindole series focused on 1,3-diaminocyclohexyl amide and urea substitutions on the pyrimidine-7-azaindole motif: In this work, we explored two strategies to eliminate observed aldehyde oxidase (AO)-mediated metabolism at the 2-position of these 7-azaindole analogues."
Our news journalists obtained a quote from the research from Vertex Pharmaceuticals Inc., "Substitution at the 2-position of the azaindole ring generated somewhat less potent analogues, but reduced AO-mediated metabolism. Incorporation of a ring nitrogen generated 7-azaindazole analogues that were equipotent to the parent 2-H-7azaindole, but surprisingly, did not appear to improve AO-mediated metabolism. Overall, we identified multiple 2-substituted 7azaindole analogues with enhanced AO stability and we present data for one such compound (12) that demonstrate a favorable oral pharmacokinetic profile in rodents."
According to the news editors, the research concluded: "These analogues have the potential to be further developed as anti-influenza agents for the treatment of influenza."
For more information on this research see: Novel 2-Substituted 7-Azaindole and 7-Azaindazole Analogues as Potential Antiviral Agents for the Treatment of Influenza. ACS Medicinal Chemistry Letters, 2017;8(2):261-265. ACS Medicinal Chemistry Letters can be contacted at: Amer Chemical Soc, 1155 16TH St, NW, Washington, DC 20036, USA. (American Chemical Society - www.acs.org; ACS Medicinal Chemistry Letters - www.pubs.acs.org/journal/amclct)
The news correspondents report that additional information may be obtained from U.K. Bandarage, Vertex Pharmaceut Inc, Boston, MA 02210, United States. Additional authors for this research include M.P. Clarke, E. Perola, H. Gao, M.D. Jacobs, A. Tsai, J. Gillespie, J.M. Kennedy, F. Maltais, M.W. Ledeboer, I. Davies, W.X. Gu, R.A. Byrn, K.N. Addae, H. Bennett, J.R. Leeman, S.M. Jones, C. O'Brien, C. Memmott and Bennan (see also Drugs and Therapies - Antiinfectives).
Keywords for this news article include: Boston, Massachusetts, United States, North and Central America, Influenza, Epidemiology, Drugs and Therapies, Antiinfectives, Antivirals, Vertex Pharmaceuticals Inc.
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