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High affinity phenylglycinol-based NK1 receptor antagonists

A P Owens1, T Harrison, J D Moseley

  • 1Department of Medicinal Chemistry, Merck Sharp and Dohme Research Laboratories, Harlow, Essex, U.K. andrew_owens@merck.com

Bioorganic & Medicinal Chemistry Letters
|January 1, 1999
PubMed
Summary
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Researchers explored heterocyclic replacements for a key group in human NK1 (neurokinin 1) receptor antagonists. This led to the development of acyclic compounds demonstrating very high affinity for the hNK1 receptor.

Area of Science:

  • Medicinal Chemistry
  • Neuroscience
  • Pharmacology

Background:

  • The neurokinin 1 (NK1) receptor is a validated target for various therapeutic applications.
  • Previous research focused on phenylglycinol-based antagonists for the human NK1 (hNK1) receptor.

Purpose of the Study:

  • To investigate novel heterocyclic replacements for the carboxamido group in phenylglycinol-based hNK1 receptor antagonists.
  • To develop novel acyclic compounds with improved affinity for the hNK1 receptor.

Main Methods:

  • Synthesis of novel heterocyclic compounds.
  • Evaluation of binding affinity for the hNK1 receptor.

Main Results:

  • Successful identification of heterocyclic replacements for the carboxamido moiety.

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  • Development of acyclic compounds exhibiting sub-nanomolar affinity for the hNK1 receptor.

    • Conclusions:

    • Heterocyclic modifications represent a viable strategy for developing potent hNK1 receptor antagonists.
    • The identified acyclic compounds show significant potential for further therapeutic development targeting the hNK1 receptor.