许蓬, 杨瑶, 施阳, 雷平生, 刘露. (9S)-9-羟基-12-亚甲基红霉素A衍生物的合成J. 药学学报, 2007, 42(5): 497-501.
引用本文: 许蓬, 杨瑶, 施阳, 雷平生, 刘露. (9S)-9-羟基-12-亚甲基红霉素A衍生物的合成J. 药学学报, 2007, 42(5): 497-501.
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XU Peng, YANG Yao, SHI Yang, LEI Ping-sheng, LIU Lu. Synthesis of derivatives of (9S)-9-hydroxyl-12-methylene erythromycin A and their antibacterial activity in vitroJ. Acta Pharmaceutica Sinica, 2007, 42(5): 497-501.
Citation: XU Peng, YANG Yao, SHI Yang, LEI Ping-sheng, LIU Lu. Synthesis of derivatives of (9S)-9-hydroxyl-12-methylene erythromycin A and their antibacterial activity in vitroJ. Acta Pharmaceutica Sinica, 2007, 42(5): 497-501.
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(9S)-9-羟基-12-亚甲基红霉素A衍生物的合成

Synthesis of derivatives of (9S)-9-hydroxyl-12-methylene erythromycin A and their antibacterial activity in vitro

    摘要
  • 摘要: 为了合成具有抗菌活性的红霉素衍生物，本文以红霉素A为原料，合成了6-位烯丙基取代中间体12，21-双键-2′-O,4″-O-二苯甲酰基-(9S)-9-O,11-O-异丙基-6-O-烯丙基红霉素A 12，得到(9S)-9-羟基-12-亚甲基衍生物6和6,7-去氢-(9S)-9-羟基-12-亚甲基衍生物11。经13C NMR，FAB-MS确证产物结构。所得化合物进行了体外抗菌活性测定。6和11均显示出较弱的抑菌活性。

     

    Abstract: The derivatives of (9S)-9-hydroxyl-12-methylene erythromycin A were synthesized by using erythromycin A as a starting material. An intermediate (9S)-9,11-O-isopropylidene-6-O-allyl-2′,4″-O-bis(benzoyl)-12,21-anhydro erythromycin A 12 was obtained. The antibacterial activity in vitro of two compounds, 6 and 11, was tested. The preliminary biological test showed that two compounds exhibited less potent antibacterial activity in vitro.

     

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