New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine

https://doi.org/10.1016/S0960-894X(98)00181-4Get rights and content

Abstract

New histamine H3 receptor antagonists were developed using an acetylene moiety as a replacement for the amide-oxime functionality of verongamine 5. Optimization of receptor binding was performed by following aliphatic Topliss tree guidelines. These new H3 ligands demonstrate excellent blood-brain barrier penetration.

New histamine H3 receptor antagonists were developed using an acetylene moiety as a replacement for the amide-oxime functionality of verongamine. The receptor binding affinities of these compounds were optimized. Ligand 14 demonstrated excellent blood-brain barrier penetration.

  1. Download : Download full-size image

References (17)

  • H. Van der Goot et al.

    Eur. J. Med. Chem.

    (1992)
  • C.R. Ganellin et al.

    Bioorg. Med. Chem. Lett.

    (1992)
  • S.J. Taylor et al.

    Biochem. Pharmacol.

    (1992)
  • J.M. Arrang et al.

    Nature

    (1987)
  • R. Leurs et al.

    Prog. Drug Res.

    (1995)
  • H. Stark et al.

    Drugs Future

    (1996)
  • J.G. Phillips et al.
  • J.W. Clitherow et al.
There are more references available in the full text version of this article.

Cited by (15)

  • Bioactive natural products from marine sources

    2001, Studies in Natural Products Chemistry
View all citing articles on Scopus
View full text