Correlation of blood-brain penetration using structural descriptors

Bioorg Med Chem. 2006 Jul 15;14(14):4888-917. doi: 10.1016/j.bmc.2006.03.012. Epub 2006 May 11.

Abstract

Experimental blood-brain partition coefficients (logBB) for a diverse set of 113 drug molecules are correlated with computed structural descriptors using CODESSA-PRO and ISIDA programs to give statistically significant QSAR models based respectively, on molecular and on fragment descriptors. The linear correlation CODESSA-PRO five-descriptor model has correlation coefficient R2=0.781 and standard deviation s2=0.123. The 'consensus model' of ISIDA gave R2=0.872 and s2=0.047. The developed models were successfully validated using the central nervous system activity data of an external test set of 40 drug molecules.

Publication types

  • Research Support, Non-U.S. Gov't
  • Validation Study

MeSH terms

  • Algorithms
  • Animals
  • Blood-Brain Barrier / physiology*
  • Central Nervous System Agents / chemistry*
  • Central Nervous System Agents / pharmacokinetics*
  • Drug Design
  • Humans
  • Models, Biological*
  • Models, Statistical
  • Quantitative Structure-Activity Relationship
  • Software

Substances

  • Central Nervous System Agents