On February 28, 2022, Rastegari, Arezoo; Safavi, Maliheh; Vafadarnejad, Fahimeh; Najafi, Zahra; Hariri, Roshanak; Bukhari, Syed Nasir Abbas; Iraji, Aida; Edraki, Najmeh; Firuzi, Omidreza; Saeedi, Mina; Mahdavi, Mohammad; Akbarzadeh, Tahmineh published an article.Related Products of 89-77-0 The title of the article was Synthesis and evaluation of novel arylisoxazoles linked to tacrine moiety: in vitro and in vivo biological activities against Alzheimer’s disease. And the article contained the following:
Focusing on the efficient cholinesterase inhibitory activity of tacrine, design and synthesis of arylisoxazole-tacrine analogs, I [R = H, 4-F, 4-O2N, etc.; X = H, Cl] was developed. In-vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition assay confirmed high potency of the title compds I. Among them, compounds I [R = 3-MeO, X = Cl; R = 4-Cl, X = H] demonstrated high activity toward AChE and BChE with IC50 values of 0.050 and 0.039μM, resp. Both compounds I [R = 3-MeO, X = Cl; R = 4-Cl, X = H] showed very good self-induced Aβ aggregation and AChE-induced inhibitory activity (79.4 and 71.4% for compound I [R = 3-MeO, X = Cl] and 61.8 and 58.6% for compound I [R = 4-Cl, X = H], resp.). Also, I [R = 3-MeO, X = Cl] showed good anti-BACE1 activity with IC50 value of 1.65μM. The metal chelation test indicated the ability of compounds I [R = 3-MeO, X = Cl; R = 4-Cl, X = H] to chelate biometals (Zn2+, Cu2+, and Fe2+). However, they showed no significant neuroprotectivity against Aβ-induced damage in PC12 cells. Evaluation of in-vitro hepatotoxicity revealed comparable toxicity of compounds I [R = 3-MeO, X = Cl; R = 4-Cl, X = H] with tacrine. In-vivo studies by Morris water maze (MWM) task demonstrated that compound I [R = 3-MeO, X = Cl] significantly reversed scopolamine-induced memory deficit in rats. Finally, mol. docking studies of compounds I [R = 3-MeO, X = Cl; R = 4-Cl, X = H] confirmed establishment of desired interactions with the AChE, BChE, and BACE1 active sites. The experimental process involved the reaction of 2-Amino-4-chlorobenzoic acid(cas: 89-77-0).Related Products of 89-77-0
The Article related to phenyl tetrahydroacridinyl aminoethyl isoxazole preparation cholinesterase bace1 inhibition neuroprotection, mol docking sar metal chelation, alzheimer’s disease, bace1, cholinesterase, isoxazole, metal chelating, morris water maze, tacrine and other aspects.Related Products of 89-77-0
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics