title: Chemiluminescent high-throughput microassay applied to imidazo[2,1-b]thiazole derivatives as potential acetylcholinesterase and butyrylcholinesterase inhibitors.
abstract: The synthesis of a new series of imidazo[2,1-b]thiazole derivatives is described. They were tested as potential acetylcholinesterase and butyrylcholinesterase inhibitors by means of a chemiluminescent microassay. Although most of the new compounds did not show significant cholinesterase inhibition potency, three of them displayed selective antiacetylcholinesterase activity in the micromolar range.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Bologna, Via Belmeloro 6, 40126 Bologna, Italy. aldo.andreani@unibo.it
authors.forename: Aldo
authors.initials: A
authors.lastname: Andreani
authors.forename: Silvia
authors.initials: S
authors.lastname: Burnelli
authors.forename: Massimiliano
authors.initials: M
authors.lastname: Granaiola
authors.forename: Massimo
authors.initials: M
authors.lastname: Guardigli
authors.forename: Alberto
authors.initials: A
authors.lastname: Leoni
authors.forename: Alessandra
authors.initials: A
authors.lastname: Locatelli
authors.forename: Rita
authors.initials: R
authors.lastname: Morigi
authors.forename: Mirella
authors.initials: M
authors.lastname: Rambaldi
authors.forename: Manuela
authors.initials: M
authors.lastname: Rizzoli
authors.forename: Lucilla
authors.initials: L
authors.lastname: Varoli
authors.forename: Aldo
authors.initials: A
authors.lastname: Roda
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism*; D000215:Acylation; D000478:Alkylation; D000818:Animals; D001554:Benzene / Q000737:chemistry; D001665:Binding Sites; D002091:Butyrylcholinesterase / Q000378:metabolism*; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D007700:Kinetics; D008163:Luminescent Measurements; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*
chemical_list: D002800:Cholinesterase Inhibitors; D007093:Imidazoles; D013844:Thiazoles; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase; D001554:Benzene