An article Novel Molecular Hybrids of N-Benzylpiperidine and 1,3,4-Oxadiazole as Multitargeted Therapeutics to Treat Alzheimer’s Disease WOS:000491219000019 published article about BETA-AMYLOID AGGREGATION; ACETYLCHOLINESTERASE INHIBITOR; ACID-DERIVATIVES; DIRECTED LIGANDS; DESIGN; PEPTIDE; ASSAY; SITE; BUTYRYLCHOLINESTERASE; NEUROTOXICITY in [Sharma, Piyoosh; Tripathi, Avanish; Tripathi, Prabhash Nath; Shrivastava, Sushant Kumar] Banaras Hindu Univ, Indian Inst Technol, Dept Pharmaceut Engn & Technol, Varanasi 221005, Uttar Pradesh, India; [Sen Singh, Saumitra; Singh, Surya Pratap] Banaras Hindu Univ, Fac Sci, Dept Biochem, Varanasi 221005, Uttar Pradesh, India in 2019, Cited 80. The Name is 4-Nitrobenzoic acid. Through research, I have a further understanding and discovery of 62-23-7. Recommanded Product: 4-Nitrobenzoic acid
Multitargeted hybrids of N-benzylpiperidine and substituted 5-phenyl-1,3,4-oxadiazoles were designed, synthesized, and evaluated against Alzheimer’s disease (AD). Tested compounds exhibited moderate to excellent inhibition against human acetylcholinesterase (hAChE), butyrylcholinesterase (hBChE), and beta-secretase-1 (hBACE-1). The potential leads 6g and 10f exhibited balanced inhibitory profiles against all the targets, with a substantial displacement of propidium iodide from the peripheral anionic site of hAChE. Hybrids 6g and 10f also elicited favorable permeation across the blood -brain barrier and were devoid of neurotoxic liability toward SH-SYSY neuroblastoma cells. Both leads remarkably disassembled A beta aggregation in thioflavin T-based selfand AChE-induced experiments. Compounds 6g and 10f ameliorated scopolamine gamma-induced cognitive dysfunctions in the Ymaze test. The ex vivo studies of rat brain homogenates established the reduced AChE levels and antioxidant activity of both compounds. Compound 6g also elicited noteworthy improvement in A beta-induced cognitive dysfunctions in the Morris water maze test with downregulation in the expression of A beta and BACE-1 proteins corroborated by Western blot and immunohistochemical analysis. The pharmacokinetic study showed excellent oral absorption characteristics of compound 6g. The in silica molecular docking and dynamics simulation studies of lead compounds affirmed their consensual binding interactions with PAS-AChE and aspartate dyad of BACE-1.
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Reference:
Phthalazine – Wikipedia,
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