Author/Authors :
Helmut Mrozik، نويسنده , , Philip Eskola، نويسنده , , Byron H. Arison، نويسنده , , Bruce O. Linn، نويسنده , , Aino Lusi، نويسنده , , Alexander Matzuk، نويسنده , , Thomas L. Shih، نويسنده , , Maureen Tischler، نويسنده , , Frank S. Waksmunski، نويسنده , , Matthew J. Wyvratt Jr.، نويسنده , , Timothy A. Blizzard، نويسنده , , Gaye M. Margiatto، نويسنده , , Michael H. Fisher، نويسنده , , Wesley L. Shoop، نويسنده , , John R. Egerton، نويسنده ,
Abstract :
Reductive amination of 4″-oxo-5-O-tert-butyldimethylsilyl-avermectins with sodium cyanoborohydride and ammonium acetate gave an epimeric mixture of 4″-deoxy-4″-amino analogs with the epimeric, axial 4″-β-amino derivative as the major component. Acylation of the amino substituent gave highly active broad spectrum antiparasitic compounds, as determined in a sheep anthelmintic assay. 4″-Epi-acetylamino-4″-deoxyavermectin B1 (12) was selected for further antiparasitic studies and is currently under development as a novel avermectin endectocide.
