Bicyclo[3.1.0]hexyl urea melanin concentrating hormone (MCH) receptor-1 antagonists: Impacting hERG liability via aryl modifications

Mark D. McBriar, Henry Guzik, Sherry Shapiro, Ruo Xu, Jaroslava Paruchova, John W. Clader, Kim O'Neill, Brian Hawes, Steve Sorota, Michael Margulis, Kristal Raylone Tucker, Daniel J. Weston, Kathleen Cox

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Abstract

Herein, we report the discovery of an effective strategy to modulate liabilities related to affinity of previously disclosed bicyclohexane MCHR-1 antagonists for the hERG channel. This paper describes one of several strategies incorporated to limit hERG binding via modifications of a terminal aryl group in an otherwise promising bicyclohexyl urea series.

Original languageEnglish (US)
Pages (from-to)4262-4265
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number16
DOIs
StatePublished - Aug 15 2006

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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    McBriar, M. D., Guzik, H., Shapiro, S., Xu, R., Paruchova, J., Clader, J. W., O'Neill, K., Hawes, B., Sorota, S., Margulis, M., Tucker, K. R., Weston, D. J., & Cox, K. (2006). Bicyclo[3.1.0]hexyl urea melanin concentrating hormone (MCH) receptor-1 antagonists: Impacting hERG liability via aryl modifications. Bioorganic and Medicinal Chemistry Letters, 16(16), 4262-4265. https://doi.org/10.1016/j.bmcl.2006.05.069