149139-22-0Relevant academic research and scientific papers
Synthesis and evaluation of novel 2-aryl-2,5,6 7-tetrahydro-3H-thieno[2' ,3':6,7]cyclohepta[1,2-c]pyridazin-3-ones and 2-aryl-5,6-dihydrothieno[2,3-h ]cinnolin-3(2H)-ones as anxiolytics
Tanaka,Kirihara,Yasumatsu,Yakushiji,Nakao
, p. 607 - 615 (2007/10/03)
A series of 2-aryl-2,5,6,7-tetrahydro-3H-thieno[2',3':6,7]cyclohepta[1,2-c]pyridazin-3-ones and 2-aryl-5,6-dihydrothieno[2,3-h]cinnolin-3(2H)-ones were synthesized and evaluated for their affinity to benzodiazepine receptors (BZRs) in the excised brain of rats and also for their intrinsic efficacy in augmentation of the γ-aminobutyric acid-induced chloride currents in the dissociated sensory neurons of frogs. The synthesized compounds showed a high affinity to BZRs. In these compounds, the substituents at the 2-position and at either the 8- or the 9-position and the ring size of the condensed ring affected the biological activity of the compounds. Thus, an introduction of 4-methyl- or 4-chloro-substituted phenyl ring into the 2-position, an introduction of methyl or ethyl into either the 8- or the g-position, and an expansion of the 6-membered condensed ring to a 7-membered ring brought about a continuous shift of compounds from inverse to full agonists. Among the synthesized compounds, 8-(1-hydroxyethyl)-2-(4-methylphenyl)-5,6- dihydrothieno[2,3-h]cinnolin-3(2H)-one, which can be classified as a BZR partial agonist, was found to exhibit an anxioselective feature.
Fused pyridazine compound
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, (2008/06/13)
A fused pyridazine compound of the formula STR1 wherein each symbol is as defined in the description. The compounds of the present invention are useful as anxiolytic agents which selectively act on anxiety because of having less side effects (e.g. muscle-
