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Sugar-based synthesis of tamiflu and its inhibitory effects on cell secretion

机译：糖基达菲的合成及其对细胞分泌的抑制作用

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Tamiflu is currently the most effective drug for the treatment of influenza, but the insufficient supply and side-effects of this drug demand urgent solutions. We present a practical synthesis of Tamiflu by using novel synthetic routes, cheap reagents, and the abundantly available starting material D-glucal. The strategy features a Claisen rearrangement of hexose to obtain the cyclohexene backbone and introduction of diamino groups through tandem intramolecular aziridination and ring opening. In addition, this synthetic protocol allows late-stage functionalization for the flexible synthesis of Tamiflu analogues. By using the synthesized Tamiflu and its active metabolite (oseltamivir carboxylate), we inves-tigated their influences on neuroendocrine PC12 cells in various aspects. It was discovered that oseltamivir carboxylate significantly inhibits the vesicular exocytosis (regulated secretion) of PC 12 cells, and suggests a mechanism underlying the Tamiflu side-effects, in particular its possible adverse influences on neurotransmitter release in the central nervous system.
机译：达菲目前是治疗流感最有效的药物，但是这种药物的供应不足和副作用急需解决方案。我们通过使用新颖的合成途径，廉价的试剂和大量可用的起始原料D-葡萄糖，介绍了达菲的实用合成。该策略的特征在于己糖的克莱森重排以获得环己烯骨架，并通过串联的分子内叠氮和开环引入二氨基。另外，该合成方案允许后期功能化以灵活合成达菲类似物。通过使用合成的达菲及其活性代谢物（奥司他韦羧酸盐），我们从各个方面研究了它们对神经内分泌PC12细胞的影响。已发现奥司他韦羧酸盐显着抑制PC 12细胞的囊泡胞吐作用（调节分泌），并提示了达菲副作用的潜在机制，特别是其对中枢神经系统中神经递质释放的可能不利影响。

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