Close the ring to break the cycle: tandem quinolone-alkyne-cyclisation gives access to tricyclic pyrrolo[1,2-<i>a</i>]quinolin-5-ones with potent anti-protozoal activity
作者:Dávid Szamosvári、Kayla Sylvester、Philipp Schmid、Kuan-Yi Lu、Emily R. Derbyshire、Thomas Böttcher
DOI:10.1039/c9cc01689a
日期:——
We describe a tandem reaction leading to tricyclic pyrrolo[1,2-a]quinolin-5-ones with unique selectivity against the liver stage of the malaria parasite.
COMPOUND FOR USE AGAINST PATHOGENIC NEISSERIA AND HAEMOPHILUS SPECIES AND MORAXELLA CATARRHALIS
申请人:Universität Konstanz
公开号:EP3502095A1
公开(公告)日:2019-06-26
The present invention relates to a compound, which can be used in the prevention and treatment of infections with pathogenic Neisseria species, in particular N. gonorrhoeae and N. meningitidis (the gonococcus and the meningococcus, respectively), and other pathogenic bacteria (e.g. Haemophilus species or Moraxella catarrhalis ), and which can be used for disinfecting a substrate from said bacteria. Moreover, the present invention relates to a corresponding pharmaceutical composition comprising said compound.
A short and divergent route to 2-alkenyl-4-quinolones
作者:Bernhard Lohrer、Franz Bracher
DOI:10.1016/j.tetlet.2018.08.062
日期:2018.10
2-alkenyl-4-quinolones were accessed via a high-yielding, three-stepsynthesis starting from 2-methyl-4-quinolones using a one-pot phosphorylation-olefination sequence as the key step and SEM as a convenient protecting group. This protocol tolerates various functional groups and gives the target olefins with complete (E)-selectivity.