Blood–brain barrier permeability considerations for CNS-targeted compound library design

A further refinement of the concept of drug-likeness is required for compound libraries intended for central nervous system (CNS) targets to account for the limitations imposed by blood–brain barrier permeability. This review describes criteria and processes that can be applied in the de novo design...

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Veröffentlicht in:Current opinion in chemical biology 2008-06, Vol.12 (3), p.318-323
1. Verfasser: Hitchcock, Stephen A
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description A further refinement of the concept of drug-likeness is required for compound libraries intended for central nervous system (CNS) targets to account for the limitations imposed by blood–brain barrier permeability. This review describes criteria and processes that can be applied in the de novo design and assembly of libraries to increase the odds of compounds residing within CNS-accessible chemical space. A number of published examples where CNS activity and/or penetration characteristics have been a factor in library design are discussed.
doi_str_mv 10.1016/j.cbpa.2008.03.019
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subjects Animals
Blood-Brain Barrier - metabolism
Central Nervous System - drug effects
Central Nervous System - metabolism
Drug Design
Humans
Permeability
Small Molecule Libraries - metabolism
Small Molecule Libraries - pharmacology
title Blood–brain barrier permeability considerations for CNS-targeted compound library design
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