650607-40-2Relevant academic research and scientific papers
Ring opening reactions of quinoline substituted epoxides
Boa, Andrew N.,Clark, Stephen,Hirst, Paul R.,Westwood, Robert
, p. 9299 - 9302 (2003)
6-Oxiranyl- and 3-oxiranyl-2-phenylquinoline-4-carboxylic acid diisopropylamides react with secondary amines and lithium amides to give (aminohydroxyethyl)quinolines but with opposite regioselectivities. Upon epoxidation of 3-formylquinoline 2 a ~5:1 mixt
Synthesis of brequinar analogue inhibitors of malaria parasite dihydroorotate dehydrogenase
Boa, Andrew N.,Canavan, Shane P.,Hirst, Paul R.,Ramsey, Christopher,Stead, Andrew M.W.,McConkey, Glenn A.
, p. 1945 - 1967 (2007/10/03)
A series of 2-phenyl quinoline-4-carboxylic acid derivatives related to brequinar, an inhibitor of human dihydroorotate dehydrogenase (DHODH), has been prepared and evaluated as inhibitors of DHODH from the malaria parasite Plasmodium falciparum. Brequinar was essentially inactive against PfDHODH (IC50 880 μM) whereas several members of the series inhibited PfDHODH. Unexpectedly, replacement of the carboxylic acid required for brequinar to inhibit hDHODH was not essential in the diisopropylamides that inhibited PfDHODH.
