This study reports the synthesis of a series of ibuprofen derivatives, including thiosemicarbazides 4a-f, 1,3,4-oxadiazoles 5a-f, 1,3,4-thiadiazoles 6a-f, 1,2,4triazoles 7a-f, and their S-alkylated derivatives 8a-d. All of the newly synthesized derivatives were analyzed using 1 H NMR, 13 C NMR spectroscopy, and highresolution mass spectra (electron ionization) spectrometry. These synthetic molecules were examined for their in vitro baking yeast α-glucosidase and soybean 15-lipoxygenase (15-LOX) inhibition and cell viability studies. The results revealed that the compounds N-(3,4-dichlorophenyl)−5-[1-(4-isobutylphenyl)ethyl]-1,3,4oxadiazol-2-amine 5f (IC 50 3.05 ± 1.23 µM) and N-(3-fluorophenyl)-5-[1-(4isobutylphenyl)ethyl]-1,3,4-oxadiazol-2-amine 5b (IC 50 3.12 ± 1.21 µM) were the most potent with respect to the α-glucosidase enzyme while in case of 15-LOX, the compound 4-(2,4-dichlorophenyl)-1-[2-(4-isobutylphenyl)propanoyl]thiosemicarbazide 4e showed potent inhibition with an IC 50 value of 55.41 ± 0.41 µM. All these compounds were found least toxic by displaying a blood mononuclear cell viability value of 69.2%-97.8% by the MTT assay compared to the standards when assayed at 0.25 mM concentration. Molecular docking analyses were conducted to evaluate the inhibition profiles of these derivatives against the said enzymes and the data supported the in vitro profiles.
Licorice, a medicinal herb, has been found to contain various phytochemicals including flavonoids, phenolic compounds, saponins, sapogenins, pterocarpenes, coumestan derivatives, 2-arylobenzofuran derivatives, chemopreventive agents, acidic constituents and glycyrrhizin having different biological activities. Licorice is used in medical for treatment of various diseases like atherosclerosis, osteoporosis and Alzheimer’s disease. It is used as anti-inflammation, anti-ulcer, anti-cancer, anti-virus and in many other problems. It is also used as additive for flavoring candies, chewing gum and toothpaste. The roots of this plant are majorly used for extracting different phytochemicals. Various licorice species: Glycyrrhiza glabra, G. uralensis, G. inflata, G. lepidota, and G. pallidiflora contain various phytochemicals with different type of biological activities. This paper provides a brief of the bioactive constituents and biological functions of different licorice species in details.
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