Author/Authors :
Clare E. Gutteridge، نويسنده , , Daniel A. Nichols، نويسنده , , Sean M. Curtis، نويسنده , , Darshan S. Thota، نويسنده , , Joseph V. Vo، نويسنده , , Lucia Gerena، نويسنده , , Gettayacamin Montip، نويسنده , , Constance O. Asher، نويسنده , , Damaris S. Diaz، نويسنده , , Charles A. DiTusa، نويسنده , , Kirsten S. Smith، نويسنده , , Apurba K. Bhattacharjee، نويسنده ,
Abstract :
Investigation of a series of 1-phenyl-3-aryl-2-propen-1-ones resulted in the identification of nine inhibitors with submicromolar efficacy against at least one Plasmodium falciparum strain in vitro. These inhibitors were inactive when given orally in a Plasmodium berghei infected mouse model. Significant compound degradation occurred upon their exposure to a liver microsome preparation, suggesting metabolic instability may be responsible for the lack of activity in vivo.
