Author/Authors :
Peter T. Meinke، نويسنده , , Wesley L. Shoop، نويسنده , , Bruce F. Michael، نويسنده , , Timothy A. Blizzard، نويسنده , , Gerard R. Dawson، نويسنده , , Michael H. Fisher، نويسنده , , Helmut Mrozik، نويسنده ,
Abstract :
A series of gem-difluoro-avermectin derivatives was synthesized from the corresponding ketones at positions 4″, 4′, 13, and 23 using diethylaminosulfur trifluoride (DAST). These fluorinated avermectins exhibit potent antiparasitic activity in a new Haemonchus contortus larval assay and are equipotent to ivermectin. In addition, 23-gem-difluoro-ivermectin displays useful anticonvulsant activity in mouse models.
