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J Med Chem. 1992 Oct 30;35(22):4092-7.

Condensation of muscimol or thiomuscimol with aminopyridazines yields GABA-A antagonists.

Author information

1
Centre de Neurochimie du CNRS, Strasbourg, France.

Abstract

Ten analogs of muscimol and thiomuscimol in which the amino function was delocalized in an amidinic system were prepared by N2 alkylation of 6-aryl-3-aminopyridazines with (chloromethyl)isoxazole or (chloromethyl)isothiazole derivatives. These muscimol and thiomuscimol derivatives show potent binding properties for GABA-A receptors (they displace [3H]GABA and [3H]gabazine) and provoke convulsions after iv injections. They fit well with the model pharmacophore proposed by our group for the GABA-A antagonists and show similar structure-activity profiles to that of the pyridazinyl-GABAs.

PMID:
1331456
DOI:
10.1021/jm00100a015
[Indexed for MEDLINE]

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