Synthesis and biological activity of allosteric modulators of GABA B receptors part 3.3-(2,6-bis-iso-propyl-4-hydroxyphenyl)propanols

Abstract

A series of six 2,2-disubstituted 3-[3,5-di-iso-propyl-4-hydroxyphenyl] propan-1-ol derivatives have been prepared for evaluation as allosteric modulators of GABAB receptors. The activity (EC50 30 μM) was greatest for the dimethyl analogue, but the isopropylphenyl compounds were generally weaker than the corresponding t-butyl compounds. Methylation of the phenolic group led to loss of activity. ©2007 Sociedade Brasileira de Química.