Oxygenating Biocatalysts for Hydroxyl Functionalisation in Drug Discovery and Development

Area of Science:

• Biocatalysis
• Organic Synthesis
• Medicinal Chemistry

Background:

• C-H oxyfunctionalisation is a key synthetic challenge.
• Oxygenating biocatalysts (oxygenases, peroxygenases) use O2 or H2O2 for oxidation.
• Biocatalyst application in organic synthesis has grown significantly for complex compound generation.

Purpose of the Study:

• To review hydroxyl functionalisation using oxygenating biocatalysts for drug discovery and development.
• To discuss established biocatalysts (e.g., P450s, flavin-dependent monooxygenases) and their limitations.
• To cover emerging biocatalysts and their applications in late-stage functionalisation and biocatalytic cascades.

Main Methods:

• Literature review of oxygenating biocatalysts.
• Focus on hydroxyl functionalisation strategies.
• Analysis of biocatalyst applications in drug discovery.

Main Results:

• Established biocatalysts show limitations in activity, stability, and substrate scope.
• Emerging biocatalysts present viable alternatives for hydroxylation.
• Biocatalytic hydroxylation enables applications like late-stage functionalisation.

Conclusions:

• Oxygenating biocatalysts are crucial tools for drug discovery and development.
• Advancements in biocatalysis expand possibilities for complex molecule synthesis.
• Hydroxylation via biocatalysis facilitates efficient drug candidate modification.