Synthesis of derivatives of (9S)-12-methylene erythromycin and their antibacterial activity in vitro.
- Author:
Lu LIU
1
;
Yao YANG
;
Yang SHI
;
Peng XU
;
Ping-sheng LEI
Author Information
- Publication Type:Journal Article
- MeSH: Anti-Bacterial Agents; chemical synthesis; pharmacology; Erythromycin; analogs & derivatives; chemical synthesis; pharmacology; Microbial Sensitivity Tests; Staphylococcus aureus; drug effects; Staphylococcus epidermidis; Streptococcus pneumoniae; drug effects
- From: Acta Pharmaceutica Sinica 2005;40(5):423-427
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo synthesizs of derivatives of (9S)-12-methylene erythromycin possessed potent antibacterial activity.
METHODSUsing 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.
RESULTSEleven derivatives of erythromycin were synthesized. Five of them were unknown compounds.
CONCLUSIONThe preliminary biological test showed that two target compounds exhibited less potent antibacterial activity in vitro.
