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.
Copyright © 2018 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Azepines / chemistry
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Azepines / metabolism
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Azepines / pharmacology
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Dogs
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Drug Design*
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Humans
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Methylation
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Molecular Structure
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Pharmaceutical Preparations / chemistry*
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Pharmaceutical Preparations / metabolism
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Pharmacokinetics
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Pharmacology
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Piperidines / chemistry
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Piperidines / metabolism
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Piperidines / pharmacology
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Pyrimidines / chemistry
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Pyrimidines / metabolism
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Pyrimidines / pharmacology
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Rats
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Solubility
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Triazoles / chemistry
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Triazoles / metabolism
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Triazoles / pharmacology
Substances
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Azepines
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MK-6096
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Pharmaceutical Preparations
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Piperidines
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Pyrimidines
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Triazoles
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suvorexant