The thesis presented here is split between two distinct projects. The first project explores the synthesis and photophysical evaluation of a new class of BODIPY dyes with handles for functionalization. These dyes may be easily modified for use in biological systems. The BODIPY dyes were synthesized by simple modifications of reported procedures and were evaluated using luminescence and UV-visible spectroscopy. An X-ray diffraction crystal structure and 19F NMR data indicate that these dyes are rigidified by intramolecular hydrogen bonding.;The second project is directed towards studying the utility of a chelator fragment library in indentifying new metal-binding groups for metalloprotein inhibitors. The chelator fragment library was screened at high concentration in cell-free bioassays against several types of metalloenzymes to yield several new metal-binding scaffolds that result in significant enzyme inhibition. One of these scaffolds was synthetically elaborated at multiple positions to demonstrate the effect of the chelator in a fragment growth strategy.
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机译:这里介绍的论文分为两个不同的项目。第一个项目探讨了新型BODIPY染料的合成和光物理评估,该染料带有用于功能化的手柄。这些染料可以容易地改性以用于生物系统。 BODIPY染料是通过简单修改报告的方法合成的,并使用发光和紫外可见光谱进行了评估。 X射线衍射晶体结构和19 F NMR数据表明,这些染料通过分子内氢键而被硬化。;第二个项目旨在研究螯合剂片段文库在鉴定金属蛋白抑制剂的新金属结合基团中的用途。在无细胞生物测定中针对几种类型的金属酶以高浓度筛选了螯合剂片段文库,以产生几种新的金属结合支架,从而显着抑制了酶。这些支架之一在多个位置进行了合成修饰,以证明螯合剂在片段生长策略中的作用。
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