71441-76-4Relevant articles and documents
Discovery of Novel, Orally Bioavailable β-Amino Acid Azaindole Inhibitors of Influenza PB2
Farmer, Luc J.,Clark, Michael P.,Boyd, Michael J.,Perola, Emanuele,Jones, Steven M.,Tsai, Alice,Jacobs, Marc D.,Bandarage, Upul K.,Ledeboer, Mark W.,Wang, Tiansheng,Deng, Hongbo,Ledford, Brian,Gu, Wenxin,Duffy, John P.,Bethiel, Randy S.,Shannon, Dean,Byrn, Randal A.,Leeman, Joshua R.,Rijnbrand, Rene,Bennett, Hamilton B.,O’Brien, Colleen,Memmott, Christine,Nti-Addae, Kwame,Bennani, Youssef L.,Charifson, Paul S.
supporting information, p. 256 - 260 (2017/03/08)
In our efforts to develop novel small-molecule inhibitors for the treatment of influenza, we utilized molecular modeling and the X-ray crystal structure of the PB2 subunit of the influenza polymerase to optimize a series of acyclic β-amino acid inhibitors, highlighted by compound 4. Compound 4 showed good oral exposure in both rat and mouse. More importantly, it showed strong potency versus multiple influenza-A strains, including pandemic 2009 H1N1 and avian H5N1 strains and showed a strong efficacy profile in a mouse influenza model even when treatment was initiated 48 h after infection. Compound 4 offers good oral bioavailability with great potential for the treatment of both pandemic and seasonal influenza.
Process for cyclizing upsilon-chlorocarboxylic acids
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, (2008/06/13)
γ-chlorocarboxylic acid methyl or ethyl esters are cyclized to the corresponding cyclopropane carboxylic acid esters by employing the sodium or potassium alcoholate of methanol or ethanol in the presence of the same alcohol at a temperature above the boiling point of the alcohol employed.
Synthesis of Cyclopropane Derivatives from Electron-deficient Olefins and Dichloromethane via Copper(I) Catalysed Photochemical Addition followed by an Electroreductive Dehalogenation Reaction
Mitani, Michiharu,Yamamoto, Yasuo,Koyama, Kikuhiko
, p. 1446 - 1447 (2007/10/02)
The CuCl-catalysed photochemical reaction of electron-deficient olefins with dichloromethane gave 1,3-dichloro compounds, which then afforded cyclopropane derivatives by electrochemical reduction.
