120121-08-6Relevant articles and documents
Allosteric Inhibitor TREA-0236 Containing Non-hydrolysable Quinazoline-4-one for EGFR T790M/C797S Mutants Inhibition
Lee, Seoyoung,Kim, Jiwon,Duggirala, Krishna Babu,Go, Areum,Shin, Inji,Cho, Byoung Chul,Choi, Gildon,Chae, Chong Hak,Lee, Kwangho
, p. 895 - 898 (2018)
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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
