Synthesis and GABA receptor potency of 3-thiomethyl-4-(hetero)aryl-5-amino-1-phenylpyrazoles.
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.
Meegalla
Sanath K
SK
3-Dimensional Pharmaceuticals, Inc., A wholly owned Johnson & Johnson company, 665 Stockton Drive, Exton, PA 1934, USA. smeegalla@prdus.jnj.com
Doller
Dario
D
Sha
DeYou
D
Soll
Rich
R
Wisnewski
Nancy
N
Silver
Gary M
GM
Dhanoa
Dale
D
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
D007306:Insecticides; D011720:Pyrazoles; D018079:Receptors, GABA