SUCCINIMIDE DERIVATIVES .2. SYNTHESIS AND ANTIPSYCHOTIC ACTIVITY OF IPERAZINYL]BUTYL]-1,2-CIS-CYCLOHEXANEDICARBOXIMIDE (SM-9018) AND RELATED-COMPOUNDS

Cyclic imides bearing omega-(4-benzisothiazol-3-yl-1-piperazinyl) alky l moieties were synthesized and tested for antipsychotic activity. The in vitro binding affinities of these compounds were examined for dopa mine 2 (D-2) and serotonin 2 (5-HT2) receptor sites. Structure-activit y relationships within these series are discussed. One of these compou nds, iperazinyl]butyl]-1,2-cis-cyclohexanedicarboxymide (SM-9018), was found to be more potent and more selective in vivo than tiospirone in its antipsychotic activity. SM-9018 (17) is currently undergoing clin ical evaluation as a selective antipsychotic agent.