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Background  It is important to develop novel antipsychotics that can effectively treat schizophrenia with minor side-effects. The aim of our work is to develop novel antipsychotics that act on dopamine D 2  and D 3 , serotonin 5-HT 1A  and 5-HT 2A  receptors with low affinity for the serotonin 5-HT 2C  and H 1  receptors, which can effectively cure positive symptoms, negative symptoms and cognitive impairment without the weight gain side-effect.    Methodology/Principal Findings  A series of 2-substituted-5-thiopropylpiperazine (piperidine) -1,3,4-oxadiazoles derivatives have been synthesized and the target compounds were evaluated for binding affinities to D 2 , 5-HT 1A  and 5-HT 2A  receptors. Preliminary results indicated that compounds 14, 16 and 22 exhibited high affinities to D 2 , 5-HT 1A  and 5-HT 2A  receptors among these compounds. Further binding tests showed that compound 22 had high affinity for D 3  receptor, and low affinity for serotonin 5-HT 2C  and H 1  receptors. In addition, compound 22 inhibited apomorphine-induced climbing behavior and MK-801-induced hyperactivity with no extrapyramidal symptoms liability in mice. Moreover, compound 22 exhibited acceptable pharmacokinetic properties.    Conclusions/Significance  Compound 22 showed an atypical antipsychotic activity without liability for extrapyramidal symptoms. We anticipate compound 22 to be useful for developing a novel class of drug for the treatment of schizophrenia.

Synthesis and Evaluation of a Series of 2-Substituted-5-Thiopropylpiperazine (Piperidine)-1,3,4-Oxadiazoles Derivatives as Atypical Antipsychotics