Methyl-containing pharmaceuticals: Methylation in drug design |
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Authors: | Shaoyi Sun Jianmin Fu |
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Affiliation: | 1. Xenon Pharmaceuticals Inc, 200-3650 Gilmore Way, Burnaby, BC V5G 4W8, Canada;2. Pharmaron Beijing Co Ltd, 6 Taihe Road, BDA Beijing 100176 PR China |
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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. |
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Keywords: | Methyl group Methylation Lead optimization Drug design |
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