title: [Lead compound optimization strategy (4)--improving blood-brain barrier permeability through structural modification].
abstract: Blood-brain barrier is a natural protection for human body. It protects central nervous system from the interruption and damage of xenobiotics. However, it prevents potential drugs aimed at central nervous system, thus becomes an obstruction for the development of central nervous system drugs. The recent development of blood-brain barrier permeability research and several lead optimization strategies to improve blood-brain barrier permeability are reviewed. These structure optimization methods include increasing lipophilicity, reducing hydrogen bond doners, simplifying molecule, increasing rigidity, lowering polar surface area, avoiding acid group, prodrug strategy, modifying into active transporter's substrates, as well as avoiding P-glycoprotein recognized structures.
authors.forename: Yu
authors.initials: Y
authors.lastname: Hong
authors.forename: Yu
authors.initials: Y
authors.lastname: Zhou
authors.forename: Jiang
authors.initials: J
authors.lastname: Wang
authors.forename: Hong
authors.initials: H
authors.lastname: Liu
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism; D001692:Biological Transport; D001812:Blood-Brain Barrier; D002490:Central Nervous System / Q000187:drug effects*; D002491:Central Nervous System Agents / Q000493:pharmacokinetics; D015195:Drug Design; D006801:Humans; D010539:Permeability; D015262:Xenobiotics / Q000009:adverse effects
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D002491:Central Nervous System Agents; D015262:Xenobiotics