Narrow SAR in odorant sensing Orco receptor agonists

作者：Romaine Ian M; Taylor Robert W; Saidu Samsudeen P; Kim Kwangho; Sulikowski Gary A; Zwiebel Laurence J; Waterson Alex G^*

来源：Bioorganic & Medicinal Chemistry Letters, 2014, 24(12): 2613-2616.

DOI：10.1016/j.bmcl.2014.04.081

• Odorant receptor
• VUAA1
• Structure activity relationship
• Drosophila melanogaster

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.

• 出版日期2014-6-15