Ontology highlight
ABSTRACT:
SUBMITTER: Bandarage UK
PROVIDER: S-EPMC5304303 | biostudies-literature | 2017 Feb
REPOSITORIES: biostudies-literature
Bandarage Upul K UK Clark Michael P MP Perola Emanuele E Gao Huai H Jacobs Marc D MD Tsai Alice A Gillespie Jeffery J Kennedy Joseph M JM Maltais François F Ledeboer Mark W MW Davies Ioana I Gu Wenxin W Byrn Randal A RA Nti Addae Kwame K Bennett Hamilton H Leeman Joshua R JR Jones Steven M SM O'Brien Colleen C Memmott Christine C Bennani Youssef Y Charifson Paul S PS
ACS medicinal chemistry letters 20170118 2
JNJ-63623872 (<b>2</b>) 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. Substitution at the 2-posi ...[more]