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Methyl-containing pharmaceuticals: Methylation in drug design
1Xenon Pharmaceuticals Inc, 200-3650 Gilmore Way, Burnaby, BC V5G 4W8, Canada.
Bioorganic & Medicinal Chemistry Letters
|September 24, 2018
Summary
Methyl groups are crucial for optimizing drug properties like activity and solubility. This methylation strategy has proven successful in developing new drugs and clinical candidates.
Area of Science:
- Medicinal Chemistry
- Drug Design
- Pharmacology
Background:
- Methyl groups play a vital role in modifying the properties of biologically active molecules.
- Understanding these modifications is key to successful drug development.
Purpose of the Study:
- To highlight the significance of methyl groups in drug design.
- To showcase successful applications of methylation strategies in pharmaceuticals.
Main Methods:
- Review of scientific literature.
- Analysis of marketed drugs and clinical candidates incorporating methylation.
- Case study compilation of beneficial methylation strategies.
Main Results:
- Methylation significantly impacts biological activity, selectivity, solubility, and pharmacokinetic/pharmacodynamic (PK/PD) profiles.
- Numerous marketed drugs and clinical candidates demonstrate the successful application of methylation.
- The strategic use of methyl groups has led to improved drug efficacy and safety.
Conclusions:
- Methylation is a powerful and effective strategy in modern drug design.
- The incorporation of methyl groups offers a reliable approach to enhance drug properties.
- Further exploration of methylation techniques can lead to the development of next-generation therapeutics.
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