An evaluation of Minor Groove Binders as anti-fungal and anti-mycobacterial therapeutics
An evaluation of Minor Groove Binders as anti-fungal and anti-mycobacterial therapeutics
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DOI：
10.1016/j.ejmech.2017.05.039
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发表时间：
2017-08-18
影响因子：
6.7
通讯作者：
Suckling, Colin J.
中科院分区：
文献类型：
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作者：
Scott, Fraser J.;Nichol, Ryan J. O.;Suckling, Colin J.
本研究详细介绍了19个结构相关的小沟结合剂（MGBs）的合成和生物学评价，这些结合剂来自天然产物偏端霉素，旨在探索抗真菌和抗分枝杆菌活性。从这个初始设置，我们报告了几个MGB 5值得更详细的调查和优化。MGB-4、MGB-317和MGB-325对新型隐球菌的MIC（80）分别为2、4和0.25 μ g/mL。MGB-353和MGB-354对分枝杆菌M的MIC（99）为3.1 μ M。结核这些化合物的选择性和活性与它们的物理化学性质和感染因子的细胞壁/膜特性有关。(C)2017年Elsevier Masson SAS。All rights reserved.
This study details the synthesis and biological evaluation of a collection of 19 structurally related Minor Groove Binders (MGBs), derived from the natural product distamycin, which were designed to probe antifungal and antimycobacterial activity. From this initial set, we report several MGB5 that are worth more detailed investigation and optimisation. MGB-4, MGB-317 and MGB-325 have promising MIC(80)s of 2, 4 and 0.25 mu g/mL, respectively, against the fungus C neoformans. MGB-353 and MGB-354 have MIC(99)s of 3.1 mu M against the mycobacterium M. tuberculosis. The selectivity and activity of these compounds is related to their physicochemical properties and the cell wall/membrane characteristics of the infective agents. (C) 2017 Elsevier Masson SAS. All rights reserved.