Bromophenols as Candida albicans isocitrate lyase inhibitors
Bromophenols as Candida albicans isocitrate lyase inhibitors
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DOI：
10.1016/j.bmcl.2010.09.015
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发表时间：
2010-11-15
影响因子：
2.7
通讯作者：
Lee, Hyi-Seung
中科院分区：
文献类型：
--
作者：
Oh, Ki-Bong;Jeon, Heung Bae;Lee, Hyi-Seung
通过相应的苯酚类似物与溴的反应，合成了一系列新的溴苯酚。测定了合成的化合物对白色念珠菌异柠檬酸裂解酶（ICL）的抑制活性以及对革兰氏阳性和革兰氏阴性细菌和真菌的抑菌活性。在所合成的溴酚中，双（3-溴-4,5-二羟基苯基）甲烷酮（11）和（3-溴-4,5-二羟基苯基）（2,3-二溴-4,5-二羟基苯基）甲烷酮（12）对ICL具有较强的抑制活性，其抑制作用强于天然溴酚1。为了确定这些化合物抑制白色念珠菌ICL活性的基本结构要求，研究了初步的构效关系。(C) 2010 Elsevier Ltd.版权所有。
A new series of bromophenols was synthesized by reactions of corresponding phenol analogs with bromine. The synthesized compounds were tested for inhibitory activity against isocitrate lyase (ICL) of Candida albicans and antimicrobial activity against Gram-positive and, Gram-negative bacteria and fungi. Among the synthesized bromophenols, bis(3-bromo-4,5-dihydroxyphenyl)methanone (11) and (3-bromo-4,5-dihydroxyphenyl)(2,3-dibromo-4,5-dihydroxyphenyl)methanone (12) displayed potent inhibitory activities against ICL, showing a stronger inhibitory effects than were found with natural bromophenol 1. The preliminary structure-activity relationships were investigated in order to determine the essential structural requirements for the inhibitory activities of these compounds against ICL of C. albicans. (C) 2010 Elsevier Ltd. All rights reserved.