Total Synthesis and Antibacterial Activity Evaluation of Griseofamine A and 16-epi-Griseofamine A

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.