Synthesis and Evaluation of Mannitol-Based Inhibitors for Lipopolysaccharide Biosynthesis

R. Johnsson
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引用次数: 2

Abstract

Antibiotic resistance is a serious threat against humankind and the need for new therapeutics is crucial. Without working antibiotics, diseases that we thought were extinct will come back. In this paper two new mannitol bisphosphate analogs, 1,6-dideoxy-1,6-diphosphoramidate mannitol and 1,6-dideoxy-1,6-dimethansulfonamide mannitol, have been synthesized and evaluated as potential inhibitors of the enzyme GmhB in the biosynthesis of lipopolysaccharides. 1,6-Dideoxy-1,6-diphosphoramidate mannitol showed promising result in computational docking experiments, but neither phosphate analog showed activity in the Kirby-Bauer antibiotic susceptibility test.
甘露醇类脂多糖生物合成抑制剂的合成与评价
抗生素耐药性是对人类的严重威胁,对新疗法的需求至关重要。如果没有有效的抗生素,我们认为已经灭绝的疾病将会卷土重来。本文合成了两种新的甘露醇双磷酸类似物1,6-二脱氧-1,6-二磷酰胺甘露醇和1,6-二脱氧-1,6-二甲磺酰胺甘露醇,并对其作为GmhB酶在脂多糖生物合成中的潜在抑制剂进行了评价。1,6-二脱氧-1,6-二磷酰胺甘露醇在计算对接实验中显示出良好的结果,但在Kirby-Bauer抗生素敏感性试验中,两种磷酸盐类似物均未显示出活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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期刊介绍: International Journal of Medicinal Chemistry is a peer-reviewed, Open Access journal that publishes original research articles as well as review articles in all areas of chemistry associated with drug discovery, design, and synthesis. International Journal of Medicinal Chemistry is a peer-reviewed, Open Access journal that publishes original research articles as well as review articles in all areas of chemistry associated with drug discovery, design, and synthesis.
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