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Synthesis and pharmacological properties of new GABA- and TRP allosteric modulators
1 , 1 , 1, 2 , * 1
1  Department of Organic and Pharmaceutical Technologies, Odessa National Polytechnic University
2  Department of Pharmaceutical Chemistry, I.I. Mechnikov Odessa National University

Published: 02 November 2015 by MDPI in 1st International Electronic Conference on Medicinal Chemistry session ECMC-1

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.

Keywords: menthol esters, GABA, TRP, salicyloylhydrazones, pharmacological activity
Comments on this paper
George Sladkovsky
Very good and detailed presentation. Great job.

Sergiy Lozovsky
Interesting research
Interesting research

Alex Lypovets
Useful info
This is very interesting and useful information. I liked the presentation, it is very helpful and demonstrable. Thanks! Good job!

Natalie Lozitsky
Good job
Very interesting research

Dorothy Robbins
Very interesting research. Great presentation. Thank you!

Elena Werby
Interesting finding on pharmacologic effects of methyl-esters of GABA and glycine. Hope, you will continue to work in this direction.

Vernon Nellis
GABA and TRP allosteric modulator
The data regarding these compounds is very interesting. A sedative, anti-convulsant and anti-inflammatory all packed into a single paper looks like you have a busy research team.