Synthesis and GABA receptor potency of 3-thiomethyl-4-(hetero)aryl-5-amino-1-phenylpyrazoles

Sanath K Meegalla; Dario Doller; DeYou Sha; Rich Soll; Nancy Wisnewski; Gary M Silver; Dale Dhanoa

doi:10.1016/j.bmcl.2004.07.033

Synthesis and GABA receptor potency of 3-thiomethyl-4-(hetero)aryl-5-amino-1-phenylpyrazoles

Bioorg Med Chem Lett. 2004 Oct 4;14(19):4949-53. doi: 10.1016/j.bmcl.2004.07.033.

Authors

Sanath K Meegalla¹, Dario Doller, DeYou Sha, Rich Soll, Nancy Wisnewski, Gary M Silver, Dale Dhanoa

Affiliation

¹ 3-Dimensional Pharmaceuticals, Inc., A wholly owned Johnson & Johnson company, 665 Stockton Drive, Exton, PA 1934, USA. [email protected]

PMID: 15341958
DOI: 10.1016/j.bmcl.2004.07.033

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.

MeSH terms

Animals
Houseflies
Insecticides / chemical synthesis*
Insecticides / pharmacology
Mice
Pyrazoles / chemical synthesis*
Pyrazoles / metabolism
Pyrazoles / pharmacology
Receptors, GABA / drug effects*
Receptors, GABA / metabolism
Structure-Activity Relationship

Substances

Insecticides
Pyrazoles
Receptors, GABA