-SUBSTITUTED-THIOCARBAMOYL-7,8-DIAZABICYCLO[4.3.0] NON-6-ENES - EVALUATION AS BSAO INHIBITORS AND PHARMACOLOGICAL ACTIVITY SCREENING

In this study a series of -substituted-thiocarbamoyl-7,8-diazabicyclo[ 4.3.0] non-6-enes derivatives previously synthesized and separated to their stereoisomers, were evaluated as BSAO inhibitors and screened ph armacologically for antidepressant activity, effect on anxiety and exp erimental parkinsonism by in vivo tests. The title compounds caused 30 -40% inhibition irrespective of geometric isomerism as well as nature of substituent. On the other hand, their open chain derivative NBE (4- ethyl, p-methoxybenzylidenthiosemicarbazide) showed a marked enzyme in hibition and antidepressant effect. While the other group was inactive as antidepressant effect, these compounds have shown diastereoselecti ve antitremor activity by inhibiting the tremors induced by oxotremori n in mice pretreated with dopaminergic antagonist haloperidol. The tit le compounds constitutes a new class of BSAO inhibitors and may serve as usefull leads for further investigation as specific BSAO inhibitors , antiparkinson, antidepressant and anticholinergic agents.