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 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 CA 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 GABAB 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.
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* 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