title: An expedient synthesis and screening for antiacetylcholinesterase activity of piperidine embedded novel pentacyclic cage compounds.
abstract: The aim of this study was to synthesize and evaluate diazapentacyclic analogs for their acetylcholinesterase (AChE) inhibitory activity. The pentacyclic analogs were synthesized by one-pot three-component domino reactions in a microwave synthesizer. Most of the compounds exhibited moderate to good AChE inhibitory activity, compound 5i showed potent inhibitory activity with IC50 1.12 ± 0.01 µM and this may provide a new lead for developing potential inhibitors for Alzheimer's disease.
authors.forename: Raju Suresh
authors.initials: RS
authors.lastname: Kumar
authors.forename: Abdulrahman I
authors.initials: AI
authors.lastname: Almansour
authors.forename: Natarajan
authors.initials: N
authors.lastname: Arumugam
authors.forename: Hasnah
authors.initials: H
authors.lastname: Osman
authors.forename: Mohamed Ashraf
authors.initials: MA
authors.lastname: Ali
authors.forename: Alireza
authors.initials: A
authors.lastname: Basiri
authors.affiliation: Department of Chemistry, College of Sciences, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia. drrajusureshkumar@gmail.com.
authors.forename: Yalda
authors.initials: Y
authors.lastname: Kia
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism*; D001372:Aza Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D003517:Cyclopentanes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D008958:Models, Molecular; D015394:Molecular Structure; D010880:Piperidines / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D001372:Aza Compounds; D002800:Cholinesterase Inhibitors; D003517:Cyclopentanes; D010880:Piperidines; C032727:piperidine; D000110:Acetylcholinesterase