Tripathi, Avanish published the artcileDesign and development of molecular hybrids of 2-pyridylpiperazine and 5-phenyl-1,3,4-oxadiazoles as potential multifunctional agents to treat Alzheimer’s disease, SDS of cas: 86-51-1, the main research area is oxadiazole preparation Alzheimer disease docking antioxidant pharmacokinetic cholinesterase inhibitor; Acetylcholinesterase (AChE); Alzheimer’s disease; Aβ aggregation; Molecular hybridization; Multi-functional agents; β-Secretase-1 (BACE-1).
The diverse nature of Alzheimer’s disease (AD) has prompted researchers to develop multi-functional agents. Synthesized mol. hybrids of 2-pyridylpiperazine and 5-phenyl-1,3,4-oxadiazoles I (R = H, 3-Me, 2,4-dihydroxy, 3,4,5-trimethoxy, etc.) were designed. Biol. activities of synthesized compounds suggested significant and balanced inhibitory potential against target enzymes. In particular, compound I (R = 2,4-difluoro (A)) containing 2,4-difluoro substitution at terminal Ph ring considered as most potential lead with inhibition of acetylcholinesterase (hAChE, IC50 = 0.054 μM), butyrylcholinesterase (hBChE, IC50 = 0.787 μM) and beta-secretase-1 (hBACE-1, IC50 = 0.098 μM). The enzyme kinetics study of (A) against hAChE suggested a mixed type of inhibition (Ki = 0.030 μM). Also, I (R = 4-bromo) and (A) showed significant displacement of propidium iodide from the peripheral anionic site (PAS) of hAChE, excellent blood-brain barrier (BBB) permeability in parallel artificial membrane permeation assay (PAMPA), and neuroprotective ability against SH-SY5Y neuroblastoma cell lines. Further, (A) also exhibited anti-Aβ aggregation activity in self- and AChE-induced thioflavin T assay, which was ascertained by morphol. characterization by at. force microscopy (AFM). Moreover, in vivo behavioral studies signified learning and memory improvement by compound (A) in scopolamine- and Aβ-induced cognitive dysfunctions performed on Y-maze and Morris water maze. The ex vivo studies suggested decreased AChE activity and antioxidant potential of compound (A), with good oral absorption characteristics ascertained by pharmacokinetic studies.
European Journal of Medicinal Chemistry published new progress about Acute toxicity. 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, SDS of cas: 86-51-1.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem