Design, Synthesis and Biological Evaluation of Rose Bengal Analogues as SecA Inhibitors
作者:Jianmei Cui、Jinshan Jin、Ying-Hsin Hsieh、Hsiuchin Yang、Bowen Ke、Krishna Damera、Phang C. Tai、Binghe Wang
DOI:10.1002/cmdc.201300216
日期:2013.8
SecA, a key component of bacterial Sec‐dependent secretion pathway, is an attractive target for exploring novel antimicrobials. Rose bengal (RB), a polyhalogenated fluorescein derivative, was found from our previous study as a potent SecA inhibitor. Here we describe the synthesis and structure–activity relationships (SAR) of 23 RB analogues that were designed by systematical dissection of RB. Evaluation
SecA是细菌Sec依赖性分泌途径的关键组成部分,是探索新型抗菌药物的有吸引力的靶标。从我们以前的研究中发现,玫瑰孟加拉(RB)是一种多卤代荧光素衍生物,是一种有效的SecA抑制剂。在这里,我们描述了通过系统解剖RB设计的23种RB类似物的合成和构效关系(SAR)。这些类似物的评估使我们能够建立SecA抑制的初始SAR。这些SecA抑制剂的抗微生物作用已在使用大肠杆菌和枯草芽孢杆菌的实验中得到证实。