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首页> 外文期刊>Chemistry: A European journal >Efforts towards the Identification of Simpler Platensimycin AnaloguesThe Total Synthesis of Oxazinidinyl Platensimycin
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Efforts towards the Identification of Simpler Platensimycin AnaloguesThe Total Synthesis of Oxazinidinyl Platensimycin

机译：努力鉴定简单的平台霉素类似物恶嗪啶基平台霉素的全合成

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摘要

Analysis of the X-ray crystal structure of platensimycin in a complex with a mutant version of the ecFabF enzyme reveals several polar interactions between the highly polar benzoic acid moiety of 1 and the FabF residues.[1] Also, the tetracyclic core of compound 1 makes both polar and van der Waals interactions within the enzymes active site. The extensive interactions between platensimycin and the FabF enzyme account for the high affinity of platensimycin to the FabF enzyme.[1] Platensimycin has a low in vivo activity when administered by conventional routes.[1] This has been attributed to the drugs poor pharmacokinetic properties. Because of platensimycins poor pharmacokinetics, we and others have initiated programs to study the structureCactivity relationship of platensimycin with the aim of identifying parts of the molecule that are amenable to modifications or deletion without adversely affecting biological activity.[4] These studies should ultimately lead to simpler analogues that are easier to synthesize and also with enhanced pharmacokinetics.
机译：对带有ecFabF酶突变型的复合物中的新霉素的X射线晶体结构进行分析，发现1的高极性苯甲酸部分与FabF残基之间存在几种极性相互作用。[1]而且，化合物1的四环核心在酶的活性位点内既发生极性相互作用又发生范德华相互作用。板霉素与FabF酶之间的广泛相互作用说明了板霉素对FabF酶的高度亲和力。[1]当通过常规途径给药时，板霉素的体内活性较低。[1]这归因于药物不良的药代动力学性质。由于板新霉素的药代动力学较差，我们和其他一些研究人员启动了计划，研究板新霉素的structureCactivity关系，目的是鉴定分子中易于修饰或缺失而不会对生物学活性产生不利影响的部分。[4]这些研究最终应导致更简单的类似物，更易于合成，并具有更高的药代动力学。

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