Rational design in search for 5-phenylhydantoin selective 5-HT7R antagonists. Molecular modeling, synthesis and biological evaluation
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- 作者：Katarzyna Kucwaj-Brysza ; Dawid Warszyckib ; Sabina Podlewskab ; c ; Jagna Witekb ; Karolina Witeka ; Andrea Gonzá ; lez Izquierdod ; Grzegorz Satałab ; Marí ; a I. Lozad ; Annamaria Lubelskaa ; Gniewomir Latacza ; Andrzej J. Bojarskib ; Mariá ; n Castrod ; Katarzyna Kieć-Kononowicza ; Jadwiga Handzlika ; j.handzlik@uj.edu.pl" class="auth_mail" title="E-mail the corresponding author
- 关键词：Hydantoins ; Phenylpiperazines ; Virtual screening ; 5-HT7R ; 5-HT1AR ; D2R ; 5-HT7R antagonists
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：13 April 2016
- 年：2016
- 卷：112
- 期：Complete
- 页码：258-269
- 全文大小：1213 K
文摘
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Design and synthesis of new 5-arylhydantoins were performed.
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5">Molecular modeling for examination of the 5-HT7R-ligand interactions was applied.
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Affinities for 5-HT1AR, 5-HT7R, D2R in radioligand binding assay were evaluated.
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5">Antagonistic activity at 5-HT7R of the 5-arylhydantoins was experimentally verified.