Title of article :
Effect of functional group polarity on the antimalarial activity of spiro and dispiro-1,2,4-trioxolanes Original Research Article
Author/Authors :
Yuxiang Dong، نويسنده , , Yuanqing Tang، نويسنده , , Jacques Chollet، نويسنده , , Hugues Matile، نويسنده , , Sergio Wittlin، نويسنده , , Susan A. Charman، نويسنده , , William N. Charman، نويسنده , , Josefina Santo Tomas، نويسنده , , Christian Scheurer، نويسنده , , Christopher Snyder، نويسنده , , Bernard Scorneaux، نويسنده , , Saroj Bajpai، نويسنده , , Scott A. Alexander، نويسنده , , Xiaofang Wang ، نويسنده , , Maniyan Padmanilayam، نويسنده , , Srinivasa R. Cheruku، نويسنده , , Reto Brun، نويسنده , , Jonathan L. Vennerstrom، نويسنده ,
Abstract :
Based on the structures of several lipophilic trioxolane antimalarial prototypes, we set out to determine which functional groups were associated with good antimalarial profiles and identify more polar (lower Log P/Log D) lead compounds with good physicochemical properties. More lipophilic trioxolanes tended to have better oral activities than their more polar counterparts. Trioxolanes with a wide range of neutral and basic, but not acidic, functional groups had good antimalarial profiles.
Keywords :
antimalarial , Artemisinin , 4-Trioxolane , 2 , Secondary ozonide , 1
