Literature DB >> 18435937

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

Stephen A Hitchcock1.   

Abstract

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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Year:  2008        PMID: 18435937     DOI: 10.1016/j.cbpa.2008.03.019

Source DB:  PubMed          Journal:  Curr Opin Chem Biol        ISSN: 1367-5931            Impact factor:   8.822


  26 in total

1.  P2X receptor antagonists for pain management: examination of binding and physicochemical properties.

Authors:  Rebecca J Gum; Brian Wakefield; Michael F Jarvis
Journal:  Purinergic Signal       Date:  2011-11-16       Impact factor: 3.765

2.  Nantenine as an acetylcholinesterase inhibitor: SAR, enzyme kinetics and molecular modeling investigations.

Authors:  Stevan Pecic; Marie A McAnuff; Wayne W Harding
Journal:  J Enzyme Inhib Med Chem       Date:  2010-06-28       Impact factor: 5.051

3.  A new in situ brain perfusion flow correction method for lipophilic drugs based on the pH-dependent Crone-Renkin equation.

Authors:  Alex Avdeef; Na Sun
Journal:  Pharm Res       Date:  2010-11-02       Impact factor: 4.200

4.  Combined Scaffold Evaluation and Systems-Level Transcriptome-Based Analysis for Accelerated Lead Optimization Reveals Ribosomal Targeting Spirooxindole Cyclopropanes.

Authors:  Kevin X Rodriguez; Erin N Howe; Emily P Bacher; Miranda Burnette; Jennifer L Meloche; Jayda Meisel; Patricia Schnepp; Xuejuan Tan; Mayland Chang; Jeremiah Zartman; Siyuan Zhang; Brandon L Ashfeld
Journal:  ChemMedChem       Date:  2019-07-01       Impact factor: 3.466

5.  Brain penetration of colistin in mice assessed by a novel high-performance liquid chromatographic technique.

Authors:  Liang Jin; Jian Li; Roger L Nation; Joseph A Nicolazzo
Journal:  Antimicrob Agents Chemother       Date:  2009-08-10       Impact factor: 5.191

6.  Reversible dimers of the atypical antipsychotic quetiapine inhibit p-glycoprotein-mediated efflux in vitro with increased binding affinity and in situ at the blood-brain barrier.

Authors:  Dana Emmert; Christopher R Campos; David Ward; Peihua Lu; Hilda A Namanja; Kelsey Bohn; David S Miller; Frances J Sharom; Jean Chmielewski; Christine A Hrycyna
Journal:  ACS Chem Neurosci       Date:  2014-02-07       Impact factor: 4.418

7.  Impact of p-glycoprotein inhibition and lipopolysaccharide administration on blood-brain barrier transport of colistin in mice.

Authors:  Liang Jin; Jian Li; Roger L Nation; Joseph A Nicolazzo
Journal:  Antimicrob Agents Chemother       Date:  2010-11-29       Impact factor: 5.191

8.  Avoiding barriers to PET radioligand development: cellular assays of brain efflux transporters.

Authors:  Matthew D Hall; Victor W Pike
Journal:  J Nucl Med       Date:  2011-02-14       Impact factor: 10.057

Review 9.  Molecular determinants of blood-brain barrier permeation.

Authors:  Werner J Geldenhuys; Afroz S Mohammad; Chris E Adkins; Paul R Lockman
Journal:  Ther Deliv       Date:  2015-08-25

10.  Synthesis and evaluation of N-(methylthiophenyl)picolinamide derivatives as PET radioligands for metabotropic glutamate receptor subtype 4.

Authors:  Kun-Eek Kil; Pekka Poutiainen; Zhaoda Zhang; Aijun Zhu; Darshini Kuruppu; Shilpa Prabhakar; Ji-Kyung Choi; Bakhos A Tannous; Anna-Liisa Brownell
Journal:  Bioorg Med Chem Lett       Date:  2015-11-10       Impact factor: 2.823

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