Structure–activity relationships of sulfonamides derived from carvacrol and their potential for the treatment of Alzheimer's disease

Abstract

We investigated the potential of sulfonamides derived from carvacrol as candidates for treatment of Alzheimer's disease. The results are very promising for the molecular target investigated as well as for the phenotypic assays.

Antioxidant Activity, Molecular Docking, Quantum Studies and In Vivo Antinociceptive Activity of Sulfonamides Derived From Carvacrol

“…This is an important measure to check for possible false positives in pain studies, as these parameters can be easily confused with an analgesic effect of the evaluated drug and cause research bias. Thus, to examine the activity of the carvacrol derivatives on spontaneous locomotion, the open-field test was performed as described above ( Nucci-Martins et al, 2016 ; de Souza et al, 2020 ). The open-field test device was a wooden box (40 × 60 × 50 cm).…”

“… Melo et al (2010) demonstrated that doses of 12.5, 25, and 50 mg/kg of carvacrol, administered orally, have an anxiolytic effect and do not alter the locomotor activity of the animals. In a previous study, we demonstrated that some synthetic sulfonamides derived from carvacrol at a dose of 30 mg/kg, intraperitoneal (ip), are able to reduce streptozotocin-induced Alzheimer’s disease deficits, in addition to producing anxiolytic and antioxidant effects, without affecting locomotor activity of animals ( de Souza et al, 2020 ). Also, it was confirmed that carvacrol, administered orally, at single doses of 50 and 100 mg/kg, produces significant inhibition of nociception caused by chemical (formalin and acetic acid) and thermal stimulations (hot-plate test) ( Cavalcante Melo et al, 2012 ).…”

“…Sulfonamides derived from carvacrol have been investigated recently, for which antibacterial properties ( Oliveira et al, 2020 ) and potential candidates for the development of drugs for the treatment of Alzheimer's disease have been reported ( De Souza et al, 2020 ). As mentioned above and due to the analgesic and anti-inflammatory potential of carvacrol, in this research, the antinociceptive potential of these sulfonamides was investigated.…”

Ileum transcriptional response to prolonged supplementation with phytogenic product containing menthol, carvacrol and carvone

“…Carvacrol elevates vascular inflammation [ 35 ] and it is also cardioprotective [ 36 ]. Additionally, it has behavioural calming effects, most likely via inhibition of gut-brain axes [ 16 ], it is neuroprotective [ 37 ], alleviating neurodegeneration and depressive-like behaviours [ 30 ], and is considered for treatment of Alzheimer's disease [ 38 ]. Recently, carvacrol's known antiviral activity was in the spotlight again, with suggestions that it is a respectable candidate for the development of anti-COVID-19 drugs [ 39 ].…”

Carvacrol Derivatives as Antifungal Agents: Synthesis, Antimicrobial Activity and in Silico Studies on Carvacryl Esters

“…Carvacryl derivatives, either natural or synthetic, have also been employed in biological testing with vast range of activities, such as antibmicrobial, [12][13][14][15] antiinflamatory, 16 antioxidant, [17][18][19][20][21] anticancer, 17,19,20 larvicidal, 22,23 antihelmintic, 24,25 also acting as enzyme inhibitors (acetylcholinesterase and butyrylcholinesterase, 26 mushroom tyrosinase, 27 Mycobacterium tuberculosis chorismate mutase 28 ).…”