title: Synthesis and GABA receptor potency of 3-thiomethyl-4-(hetero)aryl-5-amino-1-phenylpyrazoles.
abstract: A convenient synthetic route to novel 4-arylpyrazoles is described. The potential for insecticidal activity through GABA channel blockage by this series of compounds, as well as their selectivity for insect versus mammalian receptors, are explored through in vitro and in vivo assays.
authors.affiliation: 3-Dimensional Pharmaceuticals, Inc., A wholly owned Johnson & Johnson company, 665 Stockton Drive, Exton, PA 1934, USA. smeegalla@prdus.jnj.com
authors.forename: Sanath K
authors.initials: SK
authors.lastname: Meegalla
authors.forename: Dario
authors.initials: D
authors.lastname: Doller
authors.forename: DeYou
authors.initials: D
authors.lastname: Sha
authors.forename: Rich
authors.initials: R
authors.lastname: Soll
authors.forename: Nancy
authors.initials: N
authors.lastname: Wisnewski
authors.forename: Gary M
authors.initials: GM
authors.lastname: Silver
authors.forename: Dale
authors.initials: D
authors.lastname: Dhanoa
mesh_terms: D000818:Animals; D006793:Houseflies; D007306:Insecticides / Q000138:chemical synthesis* / Q000494:pharmacology; D051379:Mice; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D018079:Receptors, GABA / Q000187:drug effects* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D007306:Insecticides; D011720:Pyrazoles; D018079:Receptors, GABA