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

被引：82

作者：

Hitchcock, Stephen A. ^{[1
]}

机构：

[1] Amgen Inc, Thousand Oaks, CA 91320 USA

来源：

CURRENT OPINION IN CHEMICAL BIOLOGY | 2008年 / 12卷 / 03期

关键词：

D O I：

10.1016/j.cbpa.2008.03.019

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 [生物化学与分子生物学]; 081704 [应用化学];

摘要：

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.

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页码：318 / 323

页数：6

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