Expanding the Build-Couple-Transform paradigm to develop highly diverse screening libraries for drug discovery Newcastle University (Chemistry), Durh

化合物文库为药物发现提供了理想的目标，但它们的构建通常依赖于一种共同的起始材料，这意味着文库缺乏支架的多样性。我们的构建-耦合-转换模式解决了这个问题，在一个中心模板上使用多个多样化反应来产生一系列支架。该项目将开发新的有机化学来建立文库，重点是饱和杂环。将对这些文库进行测试，以识别针对新蛋白质目标的攻击。该项目将提供有机合成和药物化学设计方面的理想培训，非常适合希望探索药物发现职业的学生。

Compound libraries provide ideal hits for drug discovery, but their construction usually relies on a common starting material, meaning the libraries lack scaffold diversity. Our Build-Couple-Transform paradigm addresses this, using multiple diversification reactions on a central template to produce an array of scaffolds. This project will develop new organic chemistry to build libraries, with a focus on saturated heterocycles. The libraries will be tested to identify hits against novel protein targets. The project will provide ideal training in organic synthesis and medicinal chemistry design and will be ideally suited for a student wishing to explore a career in drug discovery.