Narrow SAR in odorant sensing Orco receptor agonists

Bioorg Med Chem Lett. 2014 Jun 15;24(12):2613-6. doi: 10.1016/j.bmcl.2014.04.081. Epub 2014 Apr 29.

Abstract

The systematic exploration of a series of triazole-based agonists of the cation channel insect odorant receptor is reported. The structure-activity relationships of independent sections of the molecules are examined. Very small changes to the compound structure were found to exert a large impact on compound activity. Optimal substitutions were combined using a 'mix-and-match' strategy to produce best-in-class compounds that are capable of potently agonizing odorant receptor activity and may form the basis for the identification of a new mode of insect behavior modification.

Keywords: Drosophila melanogaster; Odorant receptor; Structure activity relationship; VUAA1.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Drosophila melanogaster / physiology*
  • Indoles / chemistry
  • Indoles / pharmacology
  • Molecular Structure
  • Receptors, Odorant / agonists*
  • Receptors, Odorant / drug effects
  • Structure-Activity Relationship
  • Triazoles / chemistry
  • Triazoles / pharmacology

Substances

  • Indoles
  • Receptors, Odorant
  • Triazoles