| Autor: |
Radomir Juza, Kristyna Stefkova, Wim Dehaen, Alena Randakova, Tomas Petrasek, Iveta Vojtechova, Tereza Kobrlova, Lenka Pulkrabkova, Lubica Muckova, Marko Mecava, Lukas Prchal, Eva Mezeiova, Kamil Musilek, Ondrej Soukup, Jan Korabecny |
| Jazyk: |
angličtina |
| Rok vydání: |
2021 |
| Předmět: |
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| Zdroj: |
Biomolecules, Vol 11, Iss 9, p 1262 (2021) |
| Druh dokumentu: |
article |
| ISSN: |
2218-273X |
| DOI: |
10.3390/biom11091262 |
| Popis: |
In this pilot study, a series of new 3,4-dihydroquinolin-2(1H)-one derivatives as potential dopamine receptor D2 (D2R) modulators were synthesized and evaluated in vitro. The preliminary structure–activity relationship disclosed that compound 5e exhibited the highest D2R affinity among the newly synthesized compounds. In addition, 5e showed a very low cytotoxic profile and a high probability to cross the blood–brain barrier, which is important considering the observed affinity. However, molecular modelling simulation revealed completely different binding mode of 5e compared to USC-D301, which might be the culprit of the reduced affinity of 5e toward D2R in comparison with USC-D301. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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