100220-48-2Relevant academic research and scientific papers
Azole antifungal compounds could have dual cholinesterase inhibitory potential according to virtual screening, enzyme kinetics, and toxicity studies of an inhouse library
Barut, Burak,Sari, Suat,Sabuncuo?lu, Suna,?zel, Arzu
, (2021/03/23)
Recent advances in cholinesterase inhibitors opened new venues for the treatment of cognitive disorders like Alzheimer's disease. Certain azole antifungals like miconazole were reported to have cholinesterase inhibitory effects and hence ameliorate cognitive deficits. In this study, we tested a set of azole antifungal derivatives selected through virtual screening of an inhouse library for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory effects. Compound 61 showed potent and selective AChE inhibition (IC50 = 8.77 μM). The study also yielded dual AChE/BChE inhibitors in addition to a number of potent AChE inhibitors. Enzyme kinetics assays revealed that AChE inhibitors were competitive inhibitors. All the active compounds were imidazole derivatives and the modeling study showed that imidazole at protonated state contributed greatly to the binding interactions with some key residues of AChE and BChE active site. The active derivatives had negligible cytotoxic effects on murine fibroblast viability. According to our results, compounds featuring the classical scaffold of azole antifungal drugs could hold high potential for anticholinesterase drug design.
MICROBIOCIDAL IMIDAZOLE DERIVATIVES
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Page/Page column 21, (2017/12/09)
Compounds of the formula (I) wherein the substituents are as defined in claim 1, are useful as a pesticides especially fungicide.
N-substituted 1-aryl-2-(1H-imidazol-1-yl)-1-ethanamines with broad spectrum in vitro antimycobacterial and antifungal activities
Fioravanti, Rossella,Biava, Mariangela,Porretta, Giulio Cesare,Artico, Marino,Lampis, Giorgio,Deidda, Delia,Pompei, Raffaello
, p. 87 - 97 (2007/10/03)
Novel broad-spectrum in vitro antimycobacterial agents, namely N-(4-biphenyl-1-ylmethyl)-1-aryl-2-(1H-imidazol-1-yl)-1-ethanamines, are described. The new derivatives are also provided with in vitro antifungal activity against a variety of pathogenic fung
