[Synthesis of derivatives of (9S)-12-methylene erythromycin and their antibacterial activity in vitro].
OBJECTIVE
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.


CONCLUSIONS
The preliminary biological test showed that two target compounds exhibited less potent antibacterial activity in vitro.
Liu
Lu
L
Institute of Material Medica, Chinese Academy of Medical Sciences, China.
Yang
Yao
Y
Shi
Yang
Y
Xu
Peng
P
Lei
Ping-sheng
PS
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004917:Erythromycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D013211:Staphylococcus aureus / Q000187:drug effects; D013212:Staphylococcus epidermidis; D013296:Streptococcus pneumoniae / Q000187:drug effects
D000900:Anti-Bacterial Agents; D004917:Erythromycin