This paper describes the design and synthesis of Strathclyde minor groove binders (S-MGBs) that have been truncated by the removal of a pyrrole ring in order to mimic the structure of the natural product, disgocidine. S-MGBs have been found to be active against many different organisms, however, selective antiparasitic activity is required. A panel of seven truncated S-MGBs was prepared and the activities examined against a number of clinically relevant organisms including several bacteria and parasites. The effect of the truncation strategy on S-MGB aggregation in aqueous environment was also investigated using 1H inspection and DOSY experiments. A lead compound, a truncated S-MGB, which possesses significant activity only against trypanosomes and Leishmania has been identified for further study and was also found to be less affected by aggregation compared to its full-length analogue.

中文翻译：

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截短的 S-MGB：朝向寄生虫特异性和低聚集化学型

本文介绍了 Strathclyde 小沟粘合剂 (S-MGB) 的设计和合成，这些粘合剂通过去除吡咯环被截短，以模仿天然产物 disgocidine 的结构。已发现 S-MGB 对许多不同的生物体具有活性，但是，需要选择性的抗寄生虫活性。准备了一组七个截短的 S-MGB，并针对许多临床相关生物体（包括几种细菌和寄生虫）检查了活性。还使用 1H 检查和 DOSY 实验研究了截断策略对水性环境中 S-MGB 聚集的影响。一种先导化合物，一种截短的 S-MGB，仅对锥虫和利什曼原虫具有显着活性已确定用于进一步研究，并且还发现与其全长类似物相比受聚集的影响较小。