Application of desirability-based multi(bi)-objective optimization in the design of selective arylpiperazine derivates for the 5-HT1A serotonin receptor

Eur J Med Chem. 2009 Dec;44(12):5045-54. doi: 10.1016/j.ejmech.2009.09.008. Epub 2009 Sep 18.

Abstract

The multiobjective optimization technique based on the desirability estimation of several interrelated responses (MOOP-DESIRE) has been recently applied to quantitative structure-activity relationship (QSAR) studies. However, the advantage of applying this new methodology to the study of selectivity and affinity to competitive targets has been little explored. We used the MOOP-DESIRE methodology and a variation of this, to study the arylpiperazine derivates that could interact with 5-HT(1A) and 5-HT(2A), serotonin receptor subtypes with the objective of designing more selective molecules for the 5-HT(1A) receptor. We did show that the model results are in agreement with the available pharmacophore descriptions, guaranteeing an appropriate structural correlation and proving the methodology, as a useful tool for the important problem of selective drug design.

MeSH terms

  • Drug Design*
  • Models, Biological*
  • Molecular Structure
  • Piperazines / chemistry*
  • Protein Binding
  • Receptor, Serotonin, 5-HT1A / chemistry*
  • Receptor, Serotonin, 5-HT2A / chemistry*

Substances

  • Piperazines
  • Receptor, Serotonin, 5-HT2A
  • Receptor, Serotonin, 5-HT1A