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首页> 外文期刊>Organic letters >Actinoallolides A-E, New Anti-trypanosomal Macrolides, Produced by an Endophytic Actinomycete, Actinoallomurus fulvus MK10-036
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Actinoallolides A-E, New Anti-trypanosomal Macrolides, Produced by an Endophytic Actinomycete, Actinoallomurus fulvus MK10-036

机译:内生放线菌Actinoallomurus fulvus MK10-036生产的放线菌内酯A-E,新的抗锥虫大环内酯类

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摘要

Five new anti-trypanosomal macrolides, actinoallolides A-E (1-5), were discovered from the cultured broth of Actinoallomurus fulvus MK10-036. The structures of the actinoallolides, including absolute stereochemistry, were elucidated by a combination of spectroscopic analyses and a series of chemical derivatization studies. Actinoallolide A showed the most potent and selective in vitro anti-trypanosomal activity without cytotoxicity. A new class of promising lead compounds was identified for the development of drugs for both sleeping sickness and Chagas disease.
机译:从培养的Actinoallomurus fulvus MK10-036的培养液中发现了五种新的抗锥虫大环内酯类,放线菌体A-E(1-5)。通过结合光谱学分析和一系列化学衍生化研究,阐明了放线all基内酯的结构,包括绝对立体化学。放线放线菌素A显示出最有力和选择性的体外抗锥虫活性,而没有细胞毒性。确定了一种新的有前途的铅化合物,用于开发治疗昏睡病和南美锥虫病的药物。

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