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Preliminary mutagenicity and genotoxicity evaluation of selected arylsulfonamide derivatives of (aryloxy)alkylamines with potential psychotropic properties

  • Microbial Genetics • Original Paper
  • Published:
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Abstract

Determination of the mutagenic and genotoxic liability of biologically active compounds is of great concern for preliminary toxicity testing and drug development. In this study, we focused on the evaluation of the mutagenic and genotoxic effects of selected arylsulfonamide derivatives of aryloxyethyl piperidines and pyrrolidines (1–8), classified as 5-HT7 receptor antagonist with antidepressant and procognitive properties, using in silico and in vitro methods: the Vibrio harveyi assay and the SOS/umu-test (umuC Easy CS test). Finally, the antimutagenic potential of tested compounds was evaluated with the V. harveyi assay. It was demonstrated that none of the examined compounds produced a positive response in in vitro assays and these results were in line with in silico prediction. Additionally, all the tested compounds demonstrated various antimutagenic potential, with compound 1 (5-chloro-N-((1-(2-phenoxyethyl)piperidin-4-yl)methyl)thiophene-2-sulfonamide) being the most active against NQNO-induced mutagenicity.

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Acknowledgments

The project was supported by Jagiellonian University Medical College (grant no. K/ZDS/004118) and partially by grant no. K/DSC/001410. We thank Prof. G. Węgrzyn for providing the bacterial strains for the experiment.

Conflict of interest

The authors declare that they have no conflict of interest.

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Authors and Affiliations

  1. Department of Pharmaceutical Biochemistry, Jagiellonian University Medical College, 9 Medyczna Street, 30-688, Krakow, Poland

    Beata Powroźnik, Karolina Słoczyńska & Elżbieta Pękala

  2. Department of Medicinal Chemistry, Jagiellonian University Medical College, 9 Medyczna Street, 30-688, Krakow, Poland

    Vittorio Canale, Katarzyna Grychowska & Paweł Zajdel

Authors
  1. Beata Powroźnik
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  2. Karolina Słoczyńska
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  3. Vittorio Canale
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  4. Katarzyna Grychowska
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  5. Paweł Zajdel
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  6. Elżbieta Pękala
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Corresponding author

Correspondence to Elżbieta Pękala.

Additional information

Communicated by: Agnieszka Szalewska-Palasz

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Powroźnik, B., Słoczyńska, K., Canale, V. et al. Preliminary mutagenicity and genotoxicity evaluation of selected arylsulfonamide derivatives of (aryloxy)alkylamines with potential psychotropic properties. J Appl Genetics 57, 263–270 (2016). https://doi.org/10.1007/s13353-015-0322-5

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  • DOI: https://doi.org/10.1007/s13353-015-0322-5

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