Blue light breaks long-standing chemistry rule, unlocking 3D drug building blocks
For more than a century, pharmaceutical companies have relied on flat structures called aromatic rings, which can help drugs bind to target sites in the body. They include benzene rings and other flat, nitrogen-containing rings. But there are limits to their usefulness.
For over a century, pharmaceutical companies have depended on flat aromatic rings to aid drug binding to targets in the body. However, their rigid shape poses challenges for fitting into three-dimensional biological targets, and they also struggle with water solubility and interactions with unintended targets. To overcome these limitations, researchers at the University of Bristol, led by Varinder Aggarwal, have developed a novel method to create 3D drug building blocks by breaking a long-standing chemistry rule.
This breakthrough involves using blue light to control the formation of rigid, three-dimensional structures, a process previously hindered by the rule-of-five. By employing a simple chemical switch and a light-absorbing photocatalyst, the team transformed basic nitrogen-containing 1,5-dienes into 3D structures that could potentially serve as alternatives to planar aromatic motifs in drug design.
This innovative approach opens up new possibilities for customizing 3D structures and accelerating the discovery of novel, structurally unique scaffolds for drug discovery.
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