Abstract:Thiosemicarbazones are a class of compounds of interest for Medicinal Chemistry, as they are structurally diverse and have numerous biological activities reported in the literature. This study describes the synthesis of seventeen thiosemicarbazones, which were investigated as potential therapeutic agents for the treatment of Alzheimer's disease through antioxidant tests and an inhibitory assay of the acetylcholinesterase enzyme. All compounds showed excellent inhibition of acetylcholinesterase and exhibited ex… Show more
“…While the m -OCH group is an electron-withdrawing substituent with negative inductive effect, the o -OCH 3 group is an electron-donating substituent with a positive resonance effect. The m -OCH 3 substituent provides easier loss of the hydrogen atom via decreased strength of the N-H bond, whereas the o -OCH 3 group has the opposite effect [45]. Compound 10 (cyclic ring) has higher antioxidant activity than compound 8 (benzyl group).…”
Section: Evaluation Of Antioxidant Activitymentioning
Schiff-base-bearing new bis(thiosemicarbazone) derivatives were prepared from terephthalaldehyde and various thiosemicarbazides. FT-IR, 1 H NMR, 13 C NMR, and UV-Vis spectroscopic methods and elemental analysis were used to elucidate the identification of the synthesized molecules. The in vitro antioxidant activity of the synthesized compounds was analysed with the 1,1-diphenyl-2-picryl hydrazyl free-radical-trapping process. The synthesized compounds exhibited lower antioxidant activity than the standard ascorbic acid. IC 50 values of the synthesized molecules measured from 3.81 ± 0.01 to 29.05 ± 0.11 µ M. Among the synthesized compounds, compound 3 had the best antioxidant activity. Moreover, this study explained the structure-activity relationship of the synthesized molecules with different substituents in radical trapping reactions.
“…While the m -OCH group is an electron-withdrawing substituent with negative inductive effect, the o -OCH 3 group is an electron-donating substituent with a positive resonance effect. The m -OCH 3 substituent provides easier loss of the hydrogen atom via decreased strength of the N-H bond, whereas the o -OCH 3 group has the opposite effect [45]. Compound 10 (cyclic ring) has higher antioxidant activity than compound 8 (benzyl group).…”
Section: Evaluation Of Antioxidant Activitymentioning
Schiff-base-bearing new bis(thiosemicarbazone) derivatives were prepared from terephthalaldehyde and various thiosemicarbazides. FT-IR, 1 H NMR, 13 C NMR, and UV-Vis spectroscopic methods and elemental analysis were used to elucidate the identification of the synthesized molecules. The in vitro antioxidant activity of the synthesized compounds was analysed with the 1,1-diphenyl-2-picryl hydrazyl free-radical-trapping process. The synthesized compounds exhibited lower antioxidant activity than the standard ascorbic acid. IC 50 values of the synthesized molecules measured from 3.81 ± 0.01 to 29.05 ± 0.11 µ M. Among the synthesized compounds, compound 3 had the best antioxidant activity. Moreover, this study explained the structure-activity relationship of the synthesized molecules with different substituents in radical trapping reactions.
“…LUMO energy was a better indicator than HOMO energy regarding acetylcholinesterase inhibitory activity, and these results are in accordance with recently published data. 30…”
We report a series of functionalized dienes as compounds of great potential in the treatment of Alzheimer's disease due to their antioxidant activity and ability to inhibit the enzyme acetylcholinesterase. The dienes tested showed high enzymatic inhibition capacity and accentuated antioxidant activity, which are comparable to or higher than the standards tested. Molecular docking studies were performed to confirm the experimental results. We also describe the correlation values between the antioxidant activity and oxidation potentials. Predicted bioactivity scores and quantum studies were also determined.
“…The H 2 O 2 scavenging activity showed by the compounds was measured spectrophotometrically using a method reported previously ( Sens et al, 2018 ). A 40 mM H 2 O 2 solution was made in phosphate buffer (pH 7.4).…”
Section: Methodsmentioning
confidence: 99%
“…Scavenging Assay-Nitric Oxide NO scavenging assay was performed using the method reported by Sens et al (2018). In this assay, sodium nitroprusside generates NO radicals (NO•) which react with oxygen to generate nitrite ions.…”
The synthesis and antioxidant, antinociceptive and antiedematogenic activities of sulfonamides derived from carvacrol—a druglike natural product—are reported. The compounds showed promising antioxidant activity, and sulfonamide derived from morpholine (S1) demonstrated excellent antinociceptive and antiedematogenic activities, with no sedation or motor impairment. The mechanism that underlies the carvacrol and derived sulfonamides’ relieving effects on pain has not yet been fully elucidated, however, this study shows that the antinociceptive activity can be partially mediated by the antagonism of glutamatergic signaling. Compound S1 presented promising efficacy and was predicted to have an appropriate medicinal chemistry profile. Thus, derivative S1 is an interesting starting point for the design of new leads for the treatment of pain and associated inflammation and prooxidative conditions.
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