77651-54-8Relevant articles and documents
ISOINDOLIN-1-ON DERIVATIVE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME AS EFFECTIVE COMPONENT FOR PREVENTING OR TREATING CANCER
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Paragraph 0092; 0093, (2021/06/25)
The present invention relates to an isoindolin-1-one derivative, a method for preparing the same, and a pharmaceutical composition comprising the same as an active ingredient for preventing or treating cancer, wherein the isoindolin-1-one derivative exhib
Novel mannich bases, 5-arylimidazolidine-2,4-dione derivatives with dual 5-HT1A receptor and serotonin transporter affinity
Czopek, Anna,Ko?aczkowski, Marcin,Bucki, Adam,Byrtus, Hanna,Paw?owski, MacIej,Siwek, Agata,Bojarski, Andrzej J.,Bednarski, Marek,Wróbel, Dagmara,Weso?owska, Anna
, p. 98 - 109 (2013/05/09)
A computer aided ligand design study of imidazolidine-2,4-dione derivatives was conducted in order to obtain compounds with dual 5-HT1A receptor and serotonin transporter (SERT) affinity. According to molecular modeling results, series of Mannich bases were chosen and synthesized. Investigated compounds were tested for 5-HT1A, 5-HT2A, α1 and SERT affinity. Two selected compounds (5, 9) were characterized in functional experiments and possessed a pharmacological profile which may enhance SERT blocking efficacy - 5-HT1A partial agonism and 5-HT2A antagonism in one molecule. Furthermore these compounds displayed satisfactory selectivity over adrenergic α1 receptors. The most promising compounds, 5-arylimidazolidine-2,4-dione derivatives with 4-(3-chlorophenyl)piperazinylmethyl moiety were tested for antidepressant and anxiolytic activity. In particular, compound 5 (5-(2-methoxyphenyl)-3-{1-[4-(3-chlorophenyl)piperazin-1-yl]methyl} -imidazolidine-2,4-dione), tested in the forced swim test in mice, exhibited a favorable antidepressant-like profile without affecting spontaneous locomotor activity. Copyright