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Synthesis of potential metal-binding group compounds to examine the zinc dependency of the GPI de-N-acetylase metalloenzyme in Trypanosoma brucei

机译:合成潜在的金属结合基化合物以检查布氏锥虫中GPI de-N-乙酰化酶金属酶的锌依赖性

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class="kwd-title">Keywords: Glycosylphosphatidylinositol (GPI) biosynthesis, Zinc metalloenzyme inhibitor, Zinc-binding group, Branched monosaccharides, Phosphatidylinositol de-N-acetylase class="head no_bottom_margin" id="idm139660720764800title">AbstractA small zinc-binding group (ZBG) library of deoxy-2-C-branched-monosaccharides, for example, 1,5-anhydroglucitols, consisting of either monodentate ligand binding carboxylic acids or bidentate ligand binding hydroxamic acids, were prepared to assess the zinc affinity of the putative metalloenzyme 2-acetamido-2-deoxy-α-d-glucopyranosyl-(1→6)-phosphatidylinositol de-N-acetylase (EC 3.5.1.89) of glycosylphosphatidylinositol biosynthesis. The N-ureido thioglucoside was also synthesised and added to the ZBG library because a previous N-ureido analogue, synthesised by us, had inhibitory activity against the aforementioned de-N-acetylase, presumably via the N-ureido motif.
机译:<!-fig ft0-> <!-fig @ position =“ anchor” mode =文章f4-> <!-fig mode =“ anchred” f5-> <!-fig / graphic | fig / alternatives / graphic mode =“ anchored” m1-> class =“ kwd-title”>关键字:糖基磷脂酰肌醇(GPI)生物合成,锌金属酶抑制剂,锌结合基,支链单糖,磷脂酰肌醇N-乙酰酶 class =“ head no_bottom_margin” id =“ idm139660720764800title”>摘要一个小的脱氧-2-C分支单糖的锌结合基(ZBG)库,例如1,5-制备由单齿配体结合的羧酸或双齿配体结合的异羟肟酸组成的脱水葡萄糖醇,以评估推定的金属酶2-乙酰氨基-2-脱氧-α-d-吡喃葡萄糖基-(1→6)-磷脂酰肌醇de的锌亲和力-N-乙酰基酶(EC 3.5.1.89)进行糖基磷脂酰肌醇生物合成。还合成了N-脲基硫葡糖苷,并将其添加到ZBG库中,因为我们合成的先前的N-脲基类似物可能通过N-脲基基团具有抑制上述脱N-乙酰基酶的活性。

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