Aim: To synthesizs of derivatives of (9S)-12-methylene erythromycin possessed potent antibacterial activity.
Methods: Using erythromycin A as a starting material, via two intermediate compounds protected 12,21-dehydroerythromycin A and 6,7: 12,21-didehydro erythromycin A, several 9-O, 11-O-ethylidene compounds were obtained. During this process, benzyl and isopropyl have been selected as the protecting group. The structures of compounds obtained were confirmed with 13C NMR and MS-FAB. Their antibacterial activity in vitro was tested.
Results: Eleven derivatives of erythromycin were synthesized. Five of them were unknown compounds.
Conclusion: The preliminary biological test showed that two target compounds exhibited less potent antibacterial activity in vitro.
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