Synthesis and biological evaluation of novel quinazoline-triazole hybrid compounds with potential use in Alzheimer’s disease

Bromodomains in Human-Immunodeficiency Virus-Associated Neurocognitive Disorders: A Model of Ferroptosis-Induced Neurodegeneration

“…They are small electrophilic molecules that comprise the common denominator of over 150 naturally occurring alkaloids with numerous biological properties ( Chen et al, 2017 ). These agents possess anti-HIV, anticancer and anti-neurodegenerative properties, implicating ELS dysfunction in these pathologies ( Colacurcio and Nixon, 2016 ; Hu et al, 2018 ; Whitton et al, 2018 ; Le-Nhat-Thuy et al, 2020 ). Indeed, the quinazolinone compound, PBT434 possess iron chelating properties suggesting that lowering this biometal may benefit the patients with these conditions ( Bailey et al, 2021 ).…”

Inhibitory potential of nitrogen, oxygen and sulfur containing heterocyclic scaffolds against acetylcholinesterase and butyrylcholinesterase

“…As expected, compounds 138 (IC 50 = 2.06 µM), 139 (IC 50 = 0.23 µM) and 140 (IC 50 = 1.10 µM) bind to both catalytic anionic site (CAS) and peripheral anionic site (PAS) in the active site of the AChE enzyme, suggesting that these compounds could act as dual binding site inhibitors. These compounds were not cytotoxic, and they also displayed appropriate physicochemical as well as pharmacokinetic profiles to be developed as new AD drug contenders 220 ( Table 5 ).…”

An Overview of the Biological Evaluation of Selected Nitrogen-Containing Heterocycle Medicinal Chemistry Compounds

“…The cell passage test demonstrated that S.aureus did not develop resistance against 30 even at sub-inhibitory concentrations. A new series of quinazoline–triazole hybrid compounds have been designed, synthesized and evaluated for their anti-AChE activity by Le-Nhat-Thuy and co-workers [ 37 ]. Most of the synthesized compounds showed moderate to good AChEI activity.…”