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2005
Pyrazole derivatives
R 0180
Synthesis and GABA Receptor Potency of 3-Thiomethyl-4-(hetero)aryl-5-ami— Novel 4-arylpyrazoles with various substitution patterns are
03- 122 no-1-phenylpyrazoles.
prepared in a short time carrying out the synthesis through a parallel synthesis format.
The key step in this strategy consists of a palladium-catalyzed cross-coupling of iodopyrazole (VII) with an appropriate arylboronic acid, e.g. (VIII), or a stannane coupling
reaction, cf. (VII)→(XI). The insecticidal activity through GABA channel blockage
and the selectivity for insect vs. mammalian receptors are examined through in vitro
and in vivo assays. High binding affinity for GABA receptors is observed for a nitrile
function at C-4. Different profiles in terms of selectivity of in vivo insecticidal action
are revealed. Compounds (IX) are flea selective, (XI) is fly selective and the chloro analogue of (VII) shows dual action. — (MEEGALLA*, S. K.; DOLLER, D.; SHA, D.;
SOLL, R.; WISNEWSKI, N.; SILVER, G. M.; DHANOA, D.; Bioorg. Med. Chem.
Lett. 14 (2004) 19, 4949-4953; 3-Dimens. Pharm., Inc., Exton, PA 19341, USA;
Eng.) — H. Hoennerscheid
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