title: Narrow SAR in odorant sensing Orco receptor agonists.
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.
authors.affiliation: Vanderbilt Institute of Chemical Biology, Vanderbilt University, Nashville, TN 37322, United States.
authors.forename: Ian M
authors.initials: IM
authors.lastname: Romaine
authors.affiliation: Department of Biological Sciences, Vanderbilt University, Nashville, TN 37322, United States.
authors.forename: Robert W
authors.initials: RW
authors.lastname: Taylor
authors.affiliation: Department of Biological Sciences, Vanderbilt University, Nashville, TN 37322, United States.
authors.forename: Samsudeen P
authors.initials: SP
authors.lastname: Saidu
authors.affiliation: Vanderbilt Institute of Chemical Biology, Vanderbilt University, Nashville, TN 37322, United States; Department of Chemistry, Vanderbilt University, Nashville, TN 37322, United States.
authors.forename: Kwangho
authors.initials: K
authors.lastname: Kim
authors.affiliation: Vanderbilt Institute of Chemical Biology, Vanderbilt University, Nashville, TN 37322, United States; Department of Chemistry, Vanderbilt University, Nashville, TN 37322, United States.
authors.forename: Gary A
authors.initials: GA
authors.lastname: Sulikowski
authors.affiliation: Vanderbilt Institute of Chemical Biology, Vanderbilt University, Nashville, TN 37322, United States; Department of Pharmacology, Vanderbilt University, Nashville, TN 37322, United States; Department of Biological Sciences, Vanderbilt University, Nashville, TN 37322, United States.
authors.forename: Laurence J
authors.initials: LJ
authors.lastname: Zwiebel
authors.affiliation: Vanderbilt Institute of Chemical Biology, Vanderbilt University, Nashville, TN 37322, United States; Department of Chemistry, Vanderbilt University, Nashville, TN 37322, United States; Department of Pharmacology, Vanderbilt University, Nashville, TN 37322, United States. Electronic address: alex.g.waterson@vanderbilt.edu.
authors.forename: Alex G
authors.initials: AG
authors.lastname: Waterson
mesh_terms: D000818:Animals; D004331:Drosophila melanogaster / Q000502:physiology*; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D018035:Receptors, Odorant / Q000819:agonists* / Q000187:drug effects; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology
chemical_list: D007211:Indoles; D018035:Receptors, Odorant; D014230:Triazoles
keywords: Drosophila melanogaster; Odorant receptor; Structure activity relationship; VUAA1