Synthesis and Biological Activity of AllostericModulators of GABAB Receptors, Part 1. N-(Phenylpropyl)-1-arylethylamines*

David I. B. Kerr; Jennifer Ong; Michael V. Perkins; Rolf H. Prager; Ni Made Puspawati

doi:10.1071/CH06163

RESEARCH ARTICLE

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Synthesis and Biological Activity of AllostericModulators of GABA_B Receptors, Part 1. N-(Phenylpropyl)-1-arylethylamines*

David I. B. Kerr ^A ^C , Jennifer Ong ^A , Michael V. Perkins ^B , Rolf H. Prager ^B ^D and Ni Made Puspawati ^B

+ Author Affiliations

- Author Affiliations

^A Department of Anaesthesia and Intensive Care, University of Adelaide, Adelaide SA 5005, Australia.

^B School of Chemistry, Physics and Earth Sciences, Flinders University, Adelaide SA 5001, Australia.

^C Deceased, July 2005.

^D Corresponding author. Email: rolf.prager@flinders.edu.au

Australian Journal of Chemistry 59(7) 445-456 https://doi.org/10.1071/CH06163
Submitted: 15 May 2006 Accepted: 5 July 2006 Published: 22 August 2006

Abstract

A series of 15 analogues of fendiline, and 34 derivatives of N-(3-phenylpropyl)-1-arylethylamine have been prepared for evaluation as positive allosteric modulators of GABA_B receptors. The most active (EC₅₀, 10 nM) was N-(3,3-diphenylpropyl)-1-(3-chloro-4-methoxyphenyl)ethylamine 6g.

Acknowledgments

N.M.P. is grateful for the award of an overseas scholarship from Austaid.

References

^* Part 2: D. I. B. Kerr, J. Khalafy, J. Ong, M. V. Perkins, R. H. Prager, N. M. Puspawati, M. Rimaz, Aust. J. Chem. 2006, 59, 457. doi:10.1071/CH06164

Synthesis and Biological Activity of AllostericModulators of GABAB Receptors, Part 1. N-(Phenylpropyl)-1-arylethylamines*

Abstract

Acknowledgments

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Synthesis and Biological Activity of AllostericModulators of GABA_B Receptors, Part 1. N-(Phenylpropyl)-1-arylethylamines*