title: Coumarins as cholinesterase inhibitors: A review.
abstract: The first report in literature of the isolation of coumarin was in the year 1820. After this report, other papers were published demonstrating the isolation and synthesis of coumarin and analogues. These compounds have been studying along the years for several different pathologies. One of these pathologies was Alzheimer's disease (AD), being the main cause of dementia in the contemporary world. There are two hypotheses to explain the pathogenesis mechanism and disease symptoms, then having the "amyloid hypothesis" and the "cholinergic hypothesis". Some drugs for AD are based on the theory of "cholinergic hypothesis", which objective is to increase the concentration of ACh in the synaptic cleft by the inhibition of cholinesterases. Over the last twenty years, many studies with coumarins compounds were reported as cholinesterases inhibitors. The aim of the present review is to discuss the studies and development of new compounds for AD treatment.
authors.affiliation: Medicinal Chemistry Group, Department of Chemistry, Military Institute of Engineering, Praça General Tibêrcio 80, 22290-270, Rio de Janeiro, Brazil; Laboratãrio de Modelagem Molecular e Pesquisa em Ciências Farmacêuticas (LAMCIFAR), Nêcleo em Ecologia e Desenvolvimento Sãcio-Ambiental de Macaé (NUPEM), Universidade Federal do Rio de Janeiro- UFRJ-Campus Macaé Professor Aloísio Teixeira, Rua São José do Barreto 764, 27965-045, Macaé, RJ, Brazil.
authors.forename: Luana G
authors.initials: LG
authors.lastname: de Souza
authors.affiliation: Laboratãrio de Modelagem Molecular e Pesquisa em Ciências Farmacêuticas (LAMCIFAR), Nêcleo em Ecologia e Desenvolvimento Sãcio-Ambiental de Macaé (NUPEM), Universidade Federal do Rio de Janeiro- UFRJ-Campus Macaé Professor Aloísio Teixeira, Rua São José do Barreto 764, 27965-045, Macaé, RJ, Brazil.
authors.forename: Magdalena N
authors.initials: MN
authors.lastname: Rennã
authors.affiliation: Medicinal Chemistry Group, Department of Chemistry, Military Institute of Engineering, Praça General Tibêrcio 80, 22290-270, Rio de Janeiro, Brazil. Electronic address: jdfv2009@gmail.com.
authors.forename: Jose D
authors.initials: JD
authors.lastname: Figueroa-Villar
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy; D002800:Cholinesterase Inhibitors / Q000737:chemistry / Q000378:metabolism* / Q000627:therapeutic use; D002802:Cholinesterases / Q000737:chemistry / Q000378:metabolism*; D003374:Coumarins / Q000138:chemical synthesis / Q000378:metabolism* / Q000627:therapeutic use; D006801:Humans; D011485:Protein Binding; D013329:Structure-Activity Relationship
chemical_list: D002800:Cholinesterase Inhibitors; D003374:Coumarins; D002802:Cholinesterases
keywords: Acetylcholinesterase; Alzheimer’s disease; Benzopyrone; Butyrylcholinesterase; Coumarin; Enzyme inhibition