10-(Alkylamino)-4H-thieno[3,4-b][1,5]benzodiazepines. A novel class of potential neuroleptic agents. - Suppr | 超能文献

10-(Alkylamino)-4H-thieno[3,4-b][1,5]benzodiazepines. A novel class of potential neuroleptic agents.

作者信息

Press J B, Hofmann C M, Eudy N H, Fanshawe W J, Day I P, Greenblatt E N, Safir S R

出版信息

J Med Chem. 1979 Jun;22(6):725-31. doi: 10.1021/jm00192a020.

DOI:10.1021/jm00192a020

PMID:37338

Abstract

An investigation of the structural requirements for CNS activity of the title compounds was undertaken. A synthesis of the precursor dihydro-10H-thieno[3,4-b][1,5]benzodiazepin-10-ones was achieved and three routes for their conversion to the title compounds were developed. The compounds were tested for neuroleptic activity by means of the blockade or d-amphetamine lethality in aggregated mice and/or effects on locomotor activity in rats. Antidepressant activity was examined using inhibition of tetrabenazine-induced depression in mice. Most of the compounds were found to be potent neuroleptic agents with several exhibiting additional antidepressant activity.

摘要

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