Let’s face it, organic chemistry can seem difficult to learn. Especially from a beginner’s point of view. Like 120-21-8, Name is 4-Diethylaminobenzaldehyde. In a document, author is Gutti, Gopichand, introducing its new discovery. Safety of 4-Diethylaminobenzaldehyde.
Alzheimer’s disease (AD) is associated with multifactorial neuropathological conditions, which include cholinergic deficit, amyloid-beta plaques formation, loss of neuronal plasticity and neuronal death. Treating such multifactorial conditions with a single target directed approach is considered to be inadequate. Accordingly, multi-target directed ligand (MTDL) strategy has been evolved as an auspicious approach for the treatment of AD. In light of that, a library of 2-substituted benzo[d]oxazol-5-amine derivatives (29-39; 86-107) was designed using the scaffold hopping guided MTDLs strategy, synthesized and evaluated through various in-vitro and in-vivo biological studies. The optimal compound 92 exhibited potent inhibitory activities against AChE (IC50 = 0.052 +/- 0.010 mu M), BuChE (IC50 = 1.085 +/- 0.035 mu M), and significant amyloid-beta aggregation (20 mu M) inhibition. The compound possessed better blood-brain barrier permeability (Pe = 10.80 +/- 0.055 x 10(-6) cm s(-1)) in PAMPA assay and neuro protective properties (40 mu M) on SH-SY5Y neuroblastoma cell lines. Furthermore, in-vivo behavioural studies were performed on Y-maze test (scopolamine-induced amnesia model) and Morris water maze test (A beta(1-42) induced ICV rat model). The compound 92, at a dose of 10 mg/kg oral administration, demonstrated a substantial improvement of the cognitive and special memory impairment. In summary, both in-vitro and in-vivo investigations evidenced that compound 92 was a potential lead for the discovery of safe and effective disease-modifying agents for AD. (C) 2019 Elsevier Masson SAS. All rights reserved.
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Reference:
Benzoxazole – Wikipedia,
,Benzoxazole | C7H5NO – PubChem