Total Synthesis and Antibacterial Activity Evaluation of Griseofamine A and 16-<i>epi</i>-Griseofamine A

Abstract

The first total synthesis of griseofamine A and its diastereomer, 16- epi-griseofamine A, is described over seven steps with yields of 23% and 7%, respectively. Their antibacterial activities are also disclosed for the first time. Griseofamine A exhibited in vitro activities against a panel of drug-resistant Gram-positive bacteria with minimum inhibitory concentration (MIC) values of 8-16 μg/mL. Notably, 16- epi-griseofamine A was 2-3 times more potent than griseofamine A with MIC values of 2-8 μg/mL.