Synthesis and Biological Activity of Allosteric Modulators of GABAB Receptors, Part 2. 3-(2,6-Bis-tert-butyl-4-hydroxyphenyl)propanols*

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

doi:10.1071/CH06164

RESEARCH ARTICLE

Synthesis and Biological Activity of Allosteric Modulators of GABA_B Receptors, Part 2. 3-(2,6-Bis-tert-butyl-4-hydroxyphenyl)propanols*

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

+ 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 Chemistry Department, Urmia University, Urmia 57154, Iran.

^D Deceased, July 2005.

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

Australian Journal of Chemistry 59(7) 457-462 https://doi.org/10.1071/CH06164
Submitted: 16 May 2006 Accepted: 5 July 2006 Published: 22 August 2006

Abstract

A series of 13 2,2-disubstituted 3-(3,5-di-t-butyl-4-hydroxyphenyl)propan-1-ol derivatives have been prepared for evaluation as allosteric modulators of GABA_B receptors. The activity (EC₅₀, 4–7 μM) was greatest for the cyclohexyl and cyclopentyl analogues.

Acknowledgments

J.K. is grateful for support from Urmia and Flinders Universities for study leave; N.M.P. is grateful to Austaid for a postgraduate scholarship.

References

^* Part 1: D. I. B. Kerr, J. Ong, M. V. Perkins, R. H. Prager, N. M. Puspawati, Aust. J. Chem. 2006, 59, 445 doi:10.1071/CH06163

Synthesis and Biological Activity of Allosteric Modulators of GABAB Receptors, Part 2. 3-(2,6-Bis-tert-butyl-4-hydroxyphenyl)propanols*

Abstract

Acknowledgments

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Synthesis and Biological Activity of Allosteric Modulators of GABA_B Receptors, Part 2. 3-(2,6-Bis-tert-butyl-4-hydroxyphenyl)propanols*