Research and development of drugs with combined pharmacological effects – those that affect the different receptor types – constitute an urgent problem of modern pharmacology. In this work we are presenting the synthesis and pharmacological investigation of some new menthol, thymol and salicylic acid derivatives designed as GABA- and TRP allosteric modulators. Our findings identified menthyl ester of GABA (2-isopropyl-5-methylcyclohexyl 4-aminobutyrate) as a compound with anticonvulsant activity over a wide range of doses: 87-1350 mg/kg, whereas menthyl ester of glycine (2-isopropyl-5-methylcyclohexyl 2-aminoacetate) shows significant sedative effect over 6 hours after oral administration at 175 mg/kg. Complex compounds obtained by SnCl4 interaction with salicyloylhydrazones have demonstrated anti-inflammatory, anxiolytic, antidepressant and analgesic activities in different models in vivo. All aforementioned compounds can be considered as those that exhibit a combined pharmacological activity due to their simultaneous binding to different receptor types.
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Synthesis and pharmacological properties of new GABA- and TRP allosteric modulators
Published: 02 November 2015 by MDPI in 1st International Electronic Conference on Medicinal Chemistry session ECMC-1
Keywords: menthol esters, GABA, TRP, salicyloylhydrazones, pharmacological activity