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

Abstract

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.