Yevich, Joseph P.; New, James S.; Smith, David W.; Lobeck, Walter G.; Catt, John D.; Minielli, Joseph L.; Eison, Michael S.; Taylor, Duncan P.; Riblet, Leslie A.; Temple, Davis L. Jr. published the artcile< Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents>, Related Products of 21725-69-9, the main research area is antipsychotic benzisothiazolylpiperazine benzisoxazolylpiperazine preparation; piperazine benzisothiazolyl benzisoxazolyl.
The title compounds e.g. I [R = H, 2-benzothiazolyl, 4-(7,9-dioxo-8-azaspiro[4.5]decane-8-yl)butyl, p-FC6H4CO(CH2)3; X = S, O], were prepared and exhibited potential antipsychotic activity on the basis of their potent affinity for dopaminergic rat membrane sites labeled with [3H]spiperone and their attenuation of conditioned avoidance responding and apomorphine-induced stereotypy in rats. Thus, 3-chloro-1,2-benzisoxazole was treated with piperazine to give I (R = H, X = S), which was treated with 8-(4-chlorobutyl)-8-azaspiro[4.5]decane-7,9-dione to give I [R = 4-(7,9-dioxo-8-azaspiro[4.5]decane-8-yl)butyl, X = S] (II). Structure-activity relationships within the series are discussed. II was active in the Sidman avoidance paradigm and blocked amphetamine-induced stereotyped behavior in dogs for up to 7 h. The compound’s lack of typical neuroleptic-like effects in the rat catalepsy test coupled with its failure to produce dopamine receptor supersensitivity following chronic administration suggests that it should not cause the movement disorders commonly associated with antipsychotic therapy. II is currently undergoing clin. evaluation in schizophrenic patients.
Journal of Medicinal Chemistry published new progress about Antipsychotics. 21725-69-9 belongs to class isoxazole, and the molecular formula is C7H5NO2, Related Products of 21725-69-9.
Referemce:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem