Synthesis and biological investigation of new 4''-malonyl tethered derivatives of erythromycin and clarithromycin.

Synthesis and biological investigation of new 4''-malonyl tethered derivatives of erythromycin and clarithromycin.
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红霉素和克拉霉素的新型4-丙二酰键系衍生物的合成和生物学研究。

DOI:
10.1016/j.bmcl.2005.12.033
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发表时间:
2006
期刊:
Bioorganic & medicinal chemistry letters.
影响因子:
--
通讯作者:
Melman,Artem
Melman,Artem
中科院分区:
--
文献类型:
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作者:
Sherman,Daniel;Xiong,Liqun;Mankin,AlexanderS;Melman,Artem

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A new approach to 4″-substituted derivatives of erythromycin and clarithromycin was developed by converting them into corresponding 4″-malonic monoesters. Subsequent carbodiimide coupling with alcohols and amines provided new macrolide derivatives that are capable of binding to 50S ribosomal subunits and inhibiting protein synthesis in cell-free system.