期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 21, 页码 6540-6548出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.08.059
关键词
Hydrogen bond; Intramolecular hydrogen bond; P-Glycoprotein; Permeability; HBA; HBD; TPSA; ATP-binding cassette
The requirement to cross a biological membrane can be a complex process especially if multidrug transporters such as P-gp must be considered. Drug partitioning into the lipid membrane and efflux by P-gp are tightly coupled processes wherein H-bonding interactions play a key role. All H-bond donors and acceptors are not equal in terms of the strength of the H-bonds that they form, hence it is important to consider their relative strength. Using various examples from literature, we illustrate the benefits of considering the relative strengths of individual H-bonds and introducing intramolecular H-bonds to increase membrane permeability and/or decrease P-gp efflux. (C) 2012 Elsevier Ltd. All rights reserved.
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