• Romaine IM, Taylor RW, Saidu SP, Kim K, Sulikowski GA, Zwiebel LJ, Waterson AG. Narrow SAR in odorant sensing Orco receptor agonists. Bioorganic & medicinal chemistry letters. 2014 Jun 15;24(12). 2613-6. PMID: 24813736 [PubMed]. PMCID: PMC4111141. NIHMSID: NIHMS590655.


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.