Benzo[d][1,3] oxathiols: synthesis and biological evaluation as potential atypical antipsychotic agents

The present research paper reports the synthesis and biological evaluation of 6-(3-substitutedpropoxyl)benzo[d][1,3]oxathiol-2-ones as potential atypical antipsychotic agents. Accordingly, 10 derivatives with either amino or aryloxy substituents were synthesized. Potential antipsychotic activity of these compounds in terms of D₂ antagonism was evaluated by their ability to inhibit apomorphine-induced climbing behavior in mice and 5-HT₂ antagonistic activity of synthesized compounds was assessed by studying inhibition of 5-HTP-induced head twitches. Non-specific D₂ blockade was evaluated by studying propensity of these compounds to produce catalepsy in mice. All the synthesized compounds were found to exhibit D₂ and 5-HT₂ antagonist activity in behavioral models. However, they also induced mild to severe catalepsy. Among the 10 compounds tested, 5b and 5e exhibited maximum ‘atypical antipsychotic activity like' profile.