title: [Application of methyl in drug design].
abstract: The methyl group plays an important role in the rational drug design. Introducing methyl into small molecules has become an important strategy of lead compound optimization. The application of methyl in drug design is reviewed in this paper. Methyl can modulate the physicochemical, pharmacodynamic, and pharmacokinetic properties by ortho effect, inductive effect, and conformational effect. It also improves the metabolic stability as a soft metabolic point. In addition, introducing methyl into drug molecules can also be applied as a strategy in new uses of old drugs and generate me-too drugs.
authors.affiliation: School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
authors.forename: Jie
authors.initials: J
authors.lastname: Lian
authors.forename: Jiang
authors.initials: J
authors.lastname: Wang
authors.forename: Hai-Feng
authors.initials: HF
authors.lastname: Sun
authors.forename: Dai-Zong
authors.initials: DZ
authors.lastname: Lin
authors.forename: Hong
authors.initials: H
authors.lastname: Liu
mesh_terms: D015195:Drug Design; D057927:Hydrophobic and Hydrophilic Interactions; D050356:Lipid Metabolism; D008745:Methylation; D004364:Pharmaceutical Preparations / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism; D012995:Solubility; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D004364:Pharmaceutical Preparations