Abstract
Title compounds 1-36 were synthesized by reacting hydrazine with aldol adducts obtained from ninhydrin and methyl or alpha methylene ketones and aldehydes. Some of them showed a low, but significant benzodiazepine receptor affinity whose variation was interpreted through a structure-activity relationships study based on qualitative correlations and Comparative Molecular Field Analysis (CoMFA). Some indeno-pyridazine derivatives were found to possess an interesting anticonvulsant activity which however does not seem simply related to the benzodiazepine receptor modulation.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Animals
-
Anticonvulsants / chemical synthesis*
-
Anticonvulsants / metabolism
-
Anticonvulsants / pharmacology
-
Brain / metabolism
-
Indenes / chemical synthesis*
-
Indenes / metabolism
-
Indenes / pharmacology
-
Male
-
Mice
-
Mice, Inbred DBA
-
Mitochondria / metabolism
-
Models, Molecular
-
Pyridazines / chemical synthesis*
-
Pyridazines / metabolism
-
Pyridazines / pharmacology
-
Radioligand Assay
-
Rats
-
Rats, Sprague-Dawley
-
Receptors, GABA-A / metabolism*
-
Structure-Activity Relationship
Substances
-
Anticonvulsants
-
Indenes
-
Pyridazines
-
Receptors, GABA-A