开发一种三氯生支架，允许在 A 环和 B 环上进行运输肽的适应性改造。
Development of a triclosan scaffold which allows for adaptations on both the A- and B-ring for transport peptides.
机构信息
School of Biomedical Sciences, University of Leeds, Leeds, UK.
出版信息
Bioorg Med Chem Lett. 2013 Jun 15;23(12):3551-5. doi: 10.1016/j.bmcl.2013.04.035. Epub 2013 Apr 24.
Abstract
The enoyl acyl-carrier protein reductase (ENR) enzyme is harbored within the apicoplast of apicomplexan parasites providing a significant challenge for drug delivery, which may be overcome through the addition of transductive peptides, which facilitates crossing the apicoplast membranes. The binding site of triclosan, a potent ENR inhibitor, is occluded from the solvent making the attachment of these linkers challenging. Herein, we have produced 3 new triclosan analogs with bulky A- and B-ring motifs, which protrude into the solvent allowing for the future attachment of molecular transporters for delivery.
摘要
烯酰基辅酶 A 还原酶（ENR）酶存在于顶复门寄生虫的质体中，这给药物输送带来了重大挑战，通过添加转导肽可以克服这一挑战，转导肽有助于穿过质体膜。三氯生是一种有效的 ENR 抑制剂，其结合位点被溶剂掩盖，使得这些接头的连接变得具有挑战性。在此，我们生成了 3 种带有大 A-和 B-环结构的新型三氯生类似物，这些结构突出到溶剂中，为未来用于输送的分子转运体的附着提供了可能。
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