Covering: 1977 to 2020The ambruticins and jerangolids are myxobacterial reduced polyketides, which are produced via highly unusual biosynthetic pathways containing a plethora of non-canonical enzymatic transformations. Since the discovery of the first congeners in the late 1970s, they have been in the focus of drug development due to their good antifungal activity and low toxicity in mammals, which result from interaction with an unusual innercellular target in fungi. Despite significant efforts, which have led to the development of various total syntheses, their structural complexity has yet avoided full exploitation of their pharmacological potential. This article summarises biological, total and semisynthetic as well as biosynthetic studies on both compounds. An outlook on the biosynthesis-based approaches to them and their derivatives is presented. Due to the structural and biosynthetic characteristics of the ambruticins and jerangolids, chemoenzymatic processes that make use of their biosynthetic pathway enzymes are particularly promising to gain efficient access to derivative libraries for structure activity relationship studies.

中文翻译：

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Ambruticins 和 jerangolids - 有效抗真菌药物候选物的化学、生物学和化学酶促合成。

涵盖时间：1977 年至 2020 年 氨溴索和 jerangolids 是粘细菌减少的聚酮化合物，它们是通过非常不寻常的生物合成途径产生的，其中包含大量非规范的酶促转化。自 1970 年代后期发现第一个同源物以来，由于它们与真菌中不寻常的细胞内靶标相互作用，它们具有良好的抗真菌活性和对哺乳动物的低毒性，因此一直是药物开发的焦点。尽管做出了巨大的努力，导致了各种全合成的发展，但它们的结构复杂性尚未充分利用其药理学潜力。本文总结了这两种化合物的生物、全合成和半合成以及生物合成研究。介绍了对它们及其衍生物的基于生物合成的方法的展望。由于 ambruticins 和 jerangolids 的结构和生物合成特性，利用其生物合成途径酶的化学酶促过程特别有希望获得有效访问衍生文库以进行结构活性关系研究。