New dual ligands for the D2 and 5-HT1A receptors from the group of 1,8-naphthyl derivatives of LCAP
Authors:
- Przemysław Zaręba,
- Jolanta Jaśkowska,
- Paweł Śliwa,
- Grzegorz Satała
Abstract
More than 300 million people are suffering from depression, one of the civilization diseases in the 21st century. Serotonin 5-HT1AR and dopamine D2R play an important role in the treatment and pathogenesis of depression. Moreover, in recent years, the efficacy of dual 5-HT1A/D2 receptors ligands has been demonstrated in the fight against depression. In this work the new bulky arylpiperazine derivatives (LCAP) were synthesized in microwave radiation field. The affinities for the selected serotonin (5-HT1A,5-HT2A,5-HT6,5-HT7) and dopamine (D2) receptors have been evaluated in vitro. Compounds 5.3a, 5.4, 5.1c, 5.3d, 5.2a are promising dual 5-HT1AR/D2R ligands. The SAR analysis were additionally supported with molecular docking studies.
- Record ID
- CUT0f1ebd311d6345f6aef47dbe905fbf90
- Publication categories
- ;
- Author
- Journal series
- Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, e-ISSN 1464-3405
- Issue year
- 2019
- Vol
- 29
- No
- 16
- Pages
- 2236-2242
- Other elements of collation
- rys.; schem.; tab.; Bibliografia (na s.) - 2241-2242; Bibliografia (liczba pozycji) - 42; Oznaczenie streszczenia - Abstr.; Data udostępnienia on-line - 2019-06-20; Numeracja w czasopiśmie - Vol. 29, Iss. 16
- Keywords in English
- serotonin receptors, 5-HT1A/D2, depression, molecular modelling, microwave-assisted
- DOI
- DOI:10.1016/j.bmcl.2019.06.029 Opening in a new tab
- URL
- https://www.sciencedirect.com/science/article/pii/S0960894X19304093 Opening in a new tab
- Related project
- Synteza i ocena aktywności nowych ligandów działających na receptory ośrodkowego układu nerwowego (oun). . Project leader at PK: , ,
Projects financed by NCRD [Projekty finansowane przez NCBiR (NCBR (] - Language
- eng (en) English
- Score (nominal)
- 70
- Additional fields
- Indeksowana w: Web of Science, Scopus
- Uniform Resource Identifier
- https://cris.pk.edu.pl/info/article/CUT0f1ebd311d6345f6aef47dbe905fbf90/
- URN
urn:pkr-prod:CUT0f1ebd311d6345f6aef47dbe905fbf90
* presented citation count is obtained through Internet information analysis, and it is close to the number calculated by the Publish or PerishOpening in a new tab system.