Repozytorium
Wyszukaj
Kolekcje
Inne
Design, Synthesis, Biological Evaluation, and Molecular Docking Study of 4,6-Dimethyl-5-aryl/alkyl-2-[2-hydroxy-3-(4-substituted-1-piperazinyl)propyl]pyrrolo[3,4-c]pyrrole-1,3(2H,5H)-diones as Anti-Inflammatory Agents with Dual Inhibition of COX and LOX
Autorzy
Rok wydania
2023
Czasopismo
Numer woluminu
16
Strony
804/1-804/26
DOI
10.3390/ph16060804
Kolekcja
Język
Angielski
Typ publikacji
Artykuł
In the present study, we characterize the biological activity of a newly designed and synthesized series of 15 compounds 2-[2-hydroxy-3-(4-substituted-1-piperazinyl)propyl] derivatives of pyrrolo[3,4-c]pyrrole 3a–3o. The compounds were obtained with good yields of pyrrolo[3,4-c]pyrrole scaffold 2a–2c with secondary amines in C2H5OH. The chemical structures of the compounds were characterized by 1H-NMR, 13C-NMR, FT-IR, and MS. All the new compounds were investigated for their potencies to inhibit the activity of three enzymes, i.e., COX-1, COX-2, and LOX, by a colorimetric inhibitor screening assay. In order to analyze the structural basis of interactions between the ligands and cyclooxygenase/lipooxygenase, experimental data were supported by the results of molecular docking simulations. The data indicate that all of the tested compounds influence the activity of COX-1, COX-2, and LOX.
Słowa kluczowe
pyrrolo[3,4-c]pyrrole, cyclooxygenase inhibition COX-1/COX-2, LOX, molecular docking, analgesic activity, anti-inflammatory, cyclic imides
Licencja otwartego dostępu
Licencja na prawach której można swobodnie kopiować, rozprowadzać, zmieniać i remiksować objęty prawem autorskim utwór (Utwór-przedmiot prawa autorskiego) pod warunkiem podania imienia i nazwiska autora utworu pierwotnego oraz źródła pochodzenia utworu.
Pełny tekst licencji: https://creativecommons.org/licenses/by/3.0/pl/legalcode
Adres publiczny
http://dx.doi.org/10.3390/ph16060804
Strona internetowa wydawcy
Podobne publikacje
COX-1/COX-2 inhibition activities and molecular docking study of newly designed and synthesized pyrrolo[3,4-c]pyrrole Mannich bases.
Redzicka Aleksandra, Szczukowski Łukasz, Kochel Andrzej, Wiatrak Benita, Gębczak Katarzyna, Czyżnikowska Żaneta
Design and synthesis of N-substituted 3,4-pyrroledicarboximides as potential anti-inflammatory agents.
Redzicka Aleksandra, Czyżnikowska Żaneta, Wiatrak Benita, Gębczak Katarzyna, Kochel Andrzej
Structure-Activity relationship of 5‑butyl‑4,6-dimethyl-2-{[4-(o-fluorophenyl)-1-piperazinyl]-2-oxoethyl}-pyrrolo[3,4-c]pyrrole-1,3(2H,5H)‑dione: An experimental and theoretical study
Redzicka Aleksandra, Wojtkowiak Kamil, Kochel Andrzej, Wiatrak Benita, Jęśkowiak-Kossakowska Izabela, Jezierska Aneta