Total Synthesis and Antibacterial Activity Evaluation of Griseofamine A and 16- epi-Griseofamine A
1State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica , Peking Union Medical College and Chinese Academy of Medical Sciences , Beijing 100050 , P. R. China.
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.
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