The latest webinar in Hypha’s popular “why bother” series – “Hydroxylating drugs: why bother?”– is now available as a recording. If you missed this webinar and would like a link to the recording, please contact us for a recording link.
Abstract: Late-stage oxidation of C-H bonds in drug compounds permits the diversification of structures to alter drug properties, without the need for de novo synthesis. The selective introduction of oxidised functionality, acting as hydrogen bond donors and acceptors in three-dimensional space, allows drug molecules to interact with hitherto unexploited sites within a target protein. Thus, pharmacological properties such as potency and selectivity can be influenced, as well as PK properties and physical attributes such as solubility and polarity.
In this webinar we explore case studies from the literature where hydroxylation has added value and resulted in lead compounds with improved properties. We’ll also examine projects in which PolyCYPs enzymes have been employed to achieve late-stage oxidation through a new process called PolarExplorer.