Antinociceptive effect of extracts and compounds from Hofmeisteria schaffneri

Synthesis, Antimicrobial Activity and in silico Studies on Thymol Esters

“…29 The esters shown no acute toxicity to mice at doses higher than 5000 mg/kg which represents good congruence and indicate the usefulness of data obtained in our in silico study.…”

“…In some Inula, Doronicum and Pulicaria species, thymyl derivatives rather than sesquiterpenoids are the major root constituents. [20][21][22][23] A review by Talavera-Aleman and collaborators 24 estimated that only 10% of known functionalized thymyl derivatives have been employed in biological testing, showing vast array of diverse activities, such as antimicrobial 4,5,22,[25][26][27] (several papers reporting inhibitory activity against plants' pathogenic fungi 22,26 ), antioxidant, 28 antinociceptive, 29 anti-parasitic (antileishmanial), 30,31 antiprotozoal, 32 insecticidal 33 and piscicidal 34 activity. The usefulness of thymyl derivatives as transdermal drug delivery enhancers has also been reported.…”

“…The usefulness of thymyl derivatives as transdermal drug delivery enhancers has also been reported. 35 There are several papers reporting isolation, synthesys 4,23,29,33,36 and biological activity 4,5,22,25,[28][29][30]33 of thymyl esters. Grodnitzky and Coats 33 have tested insecticidal activity of thymyl esters of acetic, dichloracetic, trichloroacetic, chlorodifluoroacetic, pivalic and chloropivalic acid on Musca domestica.…”

“…Kumbhar and Dewang 5 tested antifungal activity and observed structure-activity relationship, stating that thymyl ethers showed better antifungal potency over esters (thymyl acetate, benzoate, cinnamate, dithymyl malonate, succinate and glutarate) and that the addition of a methylene group or a carbon, an olefinic bond or an aromatic moiety in side chain led to compounds with improved potency over the parent compound (thymol). 5 Angeles-Lopez et al 29 have undertaken a study to establish the potential acute toxicity and the antinociceptive activity in animal models of thymyl esters of C 2 -C 6 straight chain, C 4 -C 6 acids positional isomers, diasteroisomers of 2-pentenoic, and of benzoic acid, reporting several esters with antinociceptive effect at a dose of 1 mg/kg.…”

“…Keeping in view diverse pharmacological activities of thymol [7][8][9][10][11][12][13][14][15][16][17][18][19] and preliminary results on bioactivity of thymyl derivatives 4,5,22,25,[28][29][30]33 we have set the aim of our study. By making a single modification of a phenolic functionality in thymol we have obtained a series of ester compounds (3a-t), performed their structural characterization, in vitro antimicrobial testing and in silico calculation of physico-chemical, pharmacokinetic and toxicological properties.…”