Synthesis and antimicrobial evaluation of farnesyl diphosphate mimetics
Synthesis and antimicrobial evaluation of farnesyl diphosphate mimetics
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DOI：
10.1016/s0045-2068(03)00025-7
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发表时间：
2003-02-01
影响因子：
5.1
通讯作者：
van Thiel, CF
中科院分区：
文献类型：
--
作者：
Fairlamb, IJS;Dickinson, JM;van Thiel, CF
介绍了法呢基二磷酸酯模拟物的合成和首次抗菌评价。几种类似物（10、12、13和20）是白色念珠菌、粟酒裂殖酵母和酿酒酵母的抑制剂。含有ω-苯基部分和二磷酸等排体的类似物10、12和13的活性不归因于通过角鲨烯合酶抑制甾醇生物合成。两种香叶基苯砜（14和15）是大肠杆菌的有效抑制剂。Anglycol 15对鼠伤寒沙门氏菌和铜绿假单胞菌表现出有效的活性（MIC-2 μ g/mL），并且代表了对这些细菌具有活性的第一种类型的半合成萜类烯丙基砜。(C)2003 Elsevier Science（美国）。All rights reserved.
The synthesis and first antimicrobial evaluation of farnesyl diphosphate mimetics are described. Several analogues (10, 12, 13, and 20) are inhibitors of Candida albicans, Shizosaccharomyces pombe, and Saccharomyces cerevisiae. The activities of analogues 10, 12, and 13, which contain a omega-phenyl moiety and a diphosphate isostere, are not attributable to inhibition of sterol biosynthesis via squalene synthase. Two geranyl phenylsulphones (14 and 15) are potent inhibitors of Escherichia coli. Analogue 15 exhibits potent activity towards Salmonella typhimurium and Pseudomonas aeruginosa (MIC-2 mug/mL) and represents the first type of semi-synthetic terpenoid allylic sulphone active against these bacteria. (C) 2003 Elsevier Science (USA). All rights reserved.