Lead compound optimization strategy (4)--improving blood-brain barrier permeability through structural modification / 药学学报
Acta Pharmaceutica Sinica
;
(12): 789-799, 2014.
Article
in Chinese
| WPRIM
| ID: wpr-245013
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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Permeability
/
Biological Transport
/
Pharmacokinetics
/
Blood-Brain Barrier
/
Drug Design
/
Xenobiotics
/
Central Nervous System
/
Central Nervous System Agents
/
ATP Binding Cassette Transporter, Subfamily B, Member 1
/
Metabolism
Limits:
Humans
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2014
Type:
Article
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