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Design, Synthesis and Anti-fungal Activity of the Oleanic Acid Oxime Esters and Oxime Ethers

机译:齐墩果酸肟酯和肟醚的设计,合成及抗真菌活性

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@@ Glucosamine-6 phosphate synthase (GlmS) is the first enzyme of the hexosamine biosynthetic pathway. As a checkpoint of UDP-GlcNAc synthesis, it plays a key role for the bacterial peptidoglycan, the lipopolysaccharide of Gram-negative bacteria, chitin, and mannoproteins of the fungal cell wall. This enzyme catalyzes the reaction of D-fructose-6P with glutamine to afford D-glucosamine-6P and glutamate. It is irreversible reaction and the sole biosynthetic route to GlcN6P known to date. Although the enzyme is also present in mammalian systems, substantial difference in physiological consequences of GlmS inhibition in fungi and in mammals, constitute a firm molecular basis for the selective toxicity of specific enzyme inhibitors. Recently, this enzyme has been proposed as a good and promising target for new antifungal agents.
机译:氨基葡萄糖-6磷酸合酶(GlmS)是己糖胺生物合成途径的第一个酶。作为UDP-GlcNAc合成的检查点,它对细菌肽聚糖,革兰氏阴性细菌的脂多糖,几丁质和真菌细胞壁的甘露糖蛋白起关键作用。该酶催化D-果糖-6P与谷氨酰胺的反应,得到D-葡糖胺-6P和谷氨酸。这是迄今已知的不可逆的反应和唯一的生物合成途径。尽管该酶也存在于哺乳动物系统中,但是在真菌和哺乳动物中GlmS抑制的生理后果的实质性差异构成了特定酶抑制剂选择性毒性的坚实分子基础。最近,已提出将该酶作为新型抗真菌剂的良好和有希望的靶标。

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