The C‐Glycoside Analogue of the Immunostimulant α‐Galactosylceramide (KRN7000): Synthesis and Striking Enhancement of Activity

Abstract

Which source provides the better drug? The fully synthetic C-glycoside 1 (Y=CH2) is about 1000 times more potent against malaria in mice than the corresponding O-glycoside (Y=O), which is derived from a natural product and itself known to show remarkable activity against a wide range of diseases. The results of comparative biological assays emphasize the potential of C-glycosides as therapeutic agents.