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热门药物，但它们的建设通常依赖于共同的起始材料，这意味着文库缺乏支架多样性。我们的构建-耦合-转换范式解决了这一问题，在中央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图书馆，重点是饱和杂环。这些文库将进行测试，以确定与新的蛋白质靶标的匹配。该项目将在有机合成和药物化学设计方面提供理想的培训，非常适合希望探索药物发现职业生涯的学生。

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.