Molecules (2020)
Update date:2022-09-26
Topics: Experimental
Czopek, Anna
Partyka, Anna
Bucki, Adam
Paw?owski, Maciej
Ko?aczkowski, Marcin
Siwek, Agata
G?uch-Lutwin, Monika
Koczurkiewicz, Paulina
P?kala, El?bieta
Jaromin, Anna
Tyliszczak, Bo?ena
Weso?owska, Anna
Zagórska, Agnieszka
In this study, a series of compounds derived from 4-methoxy-1H-isoindole-1,3(2H)-dione, potential ligands of phosphodiesterase 10A and serotonin receptors, were investigated as potential antipsychotics. A library of 4-methoxy-1H-isoindole-1,3(2H)-dione derivatives 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, 18 (2-[4-(1H-benzimidazol-2-yl)butyl]-4-methoxy-1H-isoindole-1,3(2H)-dione), was selected and its safety in vitro was evaluated. In order to explain the binding mode of compound 18 in the active site of the PDE10A enzyme and describe the molecular interactions responsible for its inhibition, computer-aided docking studies were performed. The potential antipsychotic properties of compound 18 in a behavioral model of schizophrenia were also investigated.
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