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5-Ht6 Receptor Antagonists. V. Structure – Activity Relationship of (4-Phenylsulfonyloxazol-5-yl)amines

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Pharmaceutical Chemistry Journal Aims and scope

Both novel and previously reported (4-phenylsulfonyloxazol-5-yl)amine derivatives containing a substituted sulfonyl group were studied in order to discover highly active 5-HT6 receptor antagonists. A new pharmacophore model of 5-HT6 receptor antagonists was proposed based on the structure—5-HT6 antagonist activity relationship. It was established that the activity of the synthesized compounds depended strongly on the nature of the amine located vicinal to the sulfonyl. The most active ligands were methyl-(4-phenylsulfonyloxazol-5-yl)amines. Replacing the methyl by a bulkier alkyl radical and conversion to tertiary amines was accompanied by a dramatic reduction of their activity for 5-HT6 receptors.

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Authors and Affiliations

  1. Chemical Diversity Research Institute, Khimki, Moscow Oblast, 141401, Russia

    A. V. Ivachtchenko, E. S. Golovina, M. G. Kadieva & O. D. Mitkin

  2. ChemDiv Inc., 6605 Nancy Ridge Drive, San Diego, CA, 92121, United States

    A. V. Ivachtchenko & I. M. Okun

Authors
  1. A. V. Ivachtchenko
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  2. E. S. Golovina
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  3. M. G. Kadieva
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  4. O. D. Mitkin
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  5. I. M. Okun
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Corresponding author

Correspondence to A. V. Ivachtchenko.

Additional information

Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 46, No. 11, pp. 7 – 14, November, 2012.

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Ivachtchenko, A.V., Golovina, E.S., Kadieva, M.G. et al. 5-Ht6 Receptor Antagonists. V. Structure – Activity Relationship of (4-Phenylsulfonyloxazol-5-yl)amines. Pharm Chem J 46, 639–646 (2013). https://doi.org/10.1007/s11094-013-0861-1

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  • DOI: https://doi.org/10.1007/s11094-013-0861-1

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