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Sulikowski Lab

Narrow SAR in odorant sensing Orco receptor agonists.

AUTHORS

Romaine IMIan M , Taylor RW Robert W , Saidu SP Samsudeen P , Kim K Kwangho , Sulikowski GA Gary A , Zwiebel LJ Laurence J , Waterson AG Alex G . Bioorganic & medicinal chemistry letters. 2014 6 15; 24(12). 2613-6

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.

Copyright © 2014 Elsevier Ltd. All rights reserved.

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.

Copyright © 2014 Elsevier Ltd. All rights reserved.