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Issue 5, 2015
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Synthesis and evaluation of amide, sulfonamide and ureabenzisoxazole derivatives as potential atypical antipsychotics

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Abstract

In this paper, we report the optimization of a series of novel, potential antipsychotic derivatives combining potent dopamine D2, D3 and serotonin 5-HT1A, 5-HT2A receptor affinities. The pharmacological features of compound 27 are a high affinity for dopamine D2, D3 and serotonin 5-HT1A, 5-HT2A receptors. Moreover it possesses low affinity for 5-HT2C and H1 receptors (to reduce the risk of obesity associated with chronic treatment) and hERG channels (to reduce the incidence of torsade des pointes). Furthermore, compound 27 inhibited apomorphine-induced climbing, MK-801-induced hyperactivity and DOI-induced head twitch without observable catalepsy at the highest dose tested in mice. Taken together, among the amide derivatives, we identified compound 27 as a potential antipsychotic lead candidate.

Graphical abstract: Synthesis and evaluation of amide, sulfonamide and urea – benzisoxazole derivatives as potential atypical antipsychotics

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Publication details

The article was received on 29 Dec 2014, accepted on 12 Feb 2015 and first published on 13 Feb 2015


Article type: Concise Article
DOI: 10.1039/C4MD00578C
Citation: Med. Chem. Commun., 2015,6, 831-838
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    Synthesis and evaluation of amide, sulfonamide and ureabenzisoxazole derivatives as potential atypical antipsychotics

    Y. Chen, Y. Lan, X. Cao, X. Xu, J. Zhang, M. Yu, X. Liu, B. Liu and G. Zhang, Med. Chem. Commun., 2015, 6, 831
    DOI: 10.1039/C4MD00578C

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