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Synthesis and biological evaluation of new multi-target 3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives with potential antidepressant effect.
Wróbel, Martyna Z; Chodkowski, Andrzej; Herold, Franciszek; Marciniak, Monika; Dawidowski, Maciej; Siwek, Agata; Starowicz, Gabriela; Stachowicz, Katarzyna; Szewczyk, Bernadeta; Nowak, Gabriel; Belka, Mariusz; Baczek, Tomasz; Satala, Grzegorz; Bojarski, Andrzej J; Turlo, Jadwiga.
Affiliation
  • Wróbel MZ; Department of Drug Technology and Pharmaceutical Biotechnology, Faculty of Pharmacy, Medical University of Warsaw, 1 Banacha Street, 02-097, Warszawa, Poland. Electronic address: martyna.wrobel@wum.edu.pl.
  • Chodkowski A; Department of Drug Technology and Pharmaceutical Biotechnology, Faculty of Pharmacy, Medical University of Warsaw, 1 Banacha Street, 02-097, Warszawa, Poland.
  • Herold F; Department of Drug Technology and Pharmaceutical Biotechnology, Faculty of Pharmacy, Medical University of Warsaw, 1 Banacha Street, 02-097, Warszawa, Poland.
  • Marciniak M; Department of Drug Technology and Pharmaceutical Biotechnology, Faculty of Pharmacy, Medical University of Warsaw, 1 Banacha Street, 02-097, Warszawa, Poland.
  • Dawidowski M; Department of Drug Technology and Pharmaceutical Biotechnology, Faculty of Pharmacy, Medical University of Warsaw, 1 Banacha Street, 02-097, Warszawa, Poland.
  • Siwek A; Department of Pharmacobiology, Faculty of Pharmacy, Jagiellonian University Medical College, 9 Medyczna Street, 30-688, Kraków, Poland.
  • Starowicz G; Department of Pharmacobiology, Faculty of Pharmacy, Jagiellonian University Medical College, 9 Medyczna Street, 30-688, Kraków, Poland.
  • Stachowicz K; Department of Neurobiology, Maj Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna Street, 31-343, Kraków, Poland.
  • Szewczyk B; Department of Neurobiology, Maj Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna Street, 31-343, Kraków, Poland.
  • Nowak G; Department of Pharmacobiology, Faculty of Pharmacy, Jagiellonian University Medical College, 9 Medyczna Street, 30-688, Kraków, Poland; Department of Neurobiology, Maj Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna Street, 31-343, Kraków, Poland.
  • Belka M; Department of Pharmaceutical Chemistry, Medical University of Gdansk, 80-416, Gdansk, Poland.
  • Baczek T; Department of Pharmaceutical Chemistry, Medical University of Gdansk, 80-416, Gdansk, Poland.
  • Satala G; Department of Medicinal Chemistry, Maj Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna Street, 31-343, Kraków, Poland.
  • Bojarski AJ; Department of Medicinal Chemistry, Maj Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna Street, 31-343, Kraków, Poland.
  • Turlo J; Department of Drug Technology and Pharmaceutical Biotechnology, Faculty of Pharmacy, Medical University of Warsaw, 1 Banacha Street, 02-097, Warszawa, Poland.
Eur J Med Chem ; 183: 111736, 2019 Dec 01.
Article in En | MEDLINE | ID: mdl-31586817
ABSTRACT
A series of novel 3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives were synthesised and evaluated for their 5-HT1A/D2/5-HT2A/5-HT6/5-HT7 receptor affinity and serotonin reuptake inhibition. Most of the evaluated compounds displayed high affinities for 5-HT1A receptors (e.g., 4cKi = 2.3 nM, 4lKi = 3.2 nM). The antidepressant activity of the selected compounds was screened in vivo using the forced swim test (FST). The results indicate that compound MW005 (agonist of the pre- and postsynaptic 5-HT1A receptor) exhibited promising affinities for the 5-HT1A/SERT/D2/5-HT6/5-HT7 receptors and showed an antidepressant-like activity in the FST model.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrrolidinones / Indoles / Antidepressive Agents Limits: Animals / Humans / Male Language: En Journal: Eur J Med Chem Year: 2019 Document type: Article
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrrolidinones / Indoles / Antidepressive Agents Limits: Animals / Humans / Male Language: En Journal: Eur J Med Chem Year: 2019 Document type: Article