Czopek, Anna; Partyka, Anna; Bucki, Adam; Pawlowski, Maciej; Kolaczkowski, Marcin; Siwek, Agata; Gluch-Lutwin, Monika; Koczurkiewicz, Paulina; Pekala, Ezzbieta; Jaromin, Anna; Tyliszczak, Bozena; Wesolowska, Anna; Zagorska, Agnieszka published an article in 2020, the title of the article was Impact of N-alkylamino substituents on serotonin receptor (5-HTR) affinity and phosphodiesterase 10A (PDE10A) inhibition of isoindole-1,3-dione derivatives.SDS of cas: 574-98-1 And the article contains the following content:
In this study, a series of compounds derived from 1H-isoindole-1,3(2H)-dione I (R = H, OMe; R1 = 1,2,3,4-tetrahydroisoquinolin-2-yl, 1,2,3,4-tetrahydroisoquinolin-2-yl, pyridin-2-yl, 1H-1,3-benzimidazol-2-yl, etc.; X = (CH2)n, n = 1-5), potential ligands of phosphodiesterase 10A and serotonin receptors, were investigated as potential antipsychotics. A library of I with various amine moieties was synthesized and examined for their phosphodiesterase 10A (PDE10A)-inhibiting properties and their 5-HT1A and 5-HT7 receptor affinities. Based on in vitro studies, the most potent compound, I [R = OMe; R1 = 1H-1,3-benzimidazol-2-yl; n = 4 (II)], was selected and its safety in vitro was evaluated. In order to explain the binding mode of compound II in the active site of the PDE10A enzyme and describe the mol. interactions responsible for its inhibition, computer-aided docking studies were performed. The potential antipsychotic properties of compound II in a behavioral model of schizophrenia were also investigated. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).SDS of cas: 574-98-1
The Article related to isoindoledione preparation phosphodiesterase inhibition serotonin receptor affinity antitumor activity, antipsychotic activity, benzimidazole derivatives, phosphodiesterase 10a, schizophrenia and other aspects.SDS of cas: 574-98-1
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary