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Review
. 2018 Nov 1;28(20):3283-3289.
doi: 10.1016/j.bmcl.2018.09.016. Epub 2018 Sep 14.

Methyl-containing pharmaceuticals: Methylation in drug design

Shaoyi Sun  1 , Jianmin Fu  2
Affiliations
Review

Methyl-containing pharmaceuticals: Methylation in drug design

Shaoyi Sun et al. Bioorg Med Chem Lett. .

Abstract

The importance of methyl groups in modulating biological activity, selectivity, solubility, metabolism and pharmacokinetic/pharmacodynamic properties of biologically active molecules is highlighted. The information compiled from selected beneficial cases, focuses mostly on marketed drugs and clinical candidates, and indicates that the methylation strategy has been successful in drug design.

Keywords: Drug design; Lead optimization; Methyl group; Methylation.

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