Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype.
Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype.
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DOI：
10.1039/d1md00110h
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发表时间：
2021-08-18
影响因子：
4.1
通讯作者：
Scott FJ
中科院分区：
文献类型：
--
作者：
Brooke DP;McGee LMC;Giordani F;Cross JM;Khalaf AI;Irving C;Gillingwater K;Shaw CD;Carter KC;Barrett MP;Suckling CJ;Scott FJ
本文介绍了斯特拉斯克莱德小沟粘合剂（S-MGBs）的设计和合成，已被截断的吡咯环的去除，以模仿天然产物，迪斯戈西定的结构。已发现S-MGB对许多不同的生物体具有活性，然而，需要选择性抗寄生虫活性。制备了一组七种截短的S-MGB，并检查了其对许多临床相关生物体（包括几种细菌和寄生虫）的活性。利用1H检测和DOSY实验研究了截短策略对S-MGB在水环境中聚集的影响。一种先导化合物，截短的S-MGB，它具有显着的活性，只对锥虫和利什曼原虫已被确定为进一步研究，也被发现是受聚集相比，其全长类似物。本文介绍了斯特拉斯克莱德小沟粘合剂（S-MGBs）的设计和合成，已被截断的吡咯环的去除，以模仿天然产物，迪斯戈西定的结构。
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. 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.
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影响因子：
4
作者：
Vingadassalon, Audrey;Lorieux, Florence;Lautru, Sylvie
通讯作者：
Lautru, Sylvie
影响因子：
6.7
作者：
Scott, Fraser J.;Nichol, Ryan J. O.;Suckling, Colin J.
通讯作者：
Suckling, Colin J.
影响因子：
7.3
作者：
Anthony, Nahoum G.;Breerl, David;Waiah, Roger D.
通讯作者：
Waiah, Roger D.
影响因子：
7.3
作者：
Giordani, Federica;Khalaf, Abedawn I.;Scott, Fraser J.
通讯作者：
Scott, Fraser J.
影响因子：
2.7
作者：
Scott, Fraser J.;Khalaf, Abedawn I.;Suckling, Colin J.
通讯作者：
Suckling, Colin J.