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Design and synthesis of N-substituted 3,4-pyrroledicarboximides as potential anti-inflammatory agents.
Autorzy
Rok wydania
2021
Czasopismo
International Journal of Molecular Sciences
Numer woluminu
22
Strony
1410/1-1410/22
DOI
10.3390/ijms22031410
Kolekcja
Język
Angielski
Typ publikacji
Artykuł
In the present paper, we describe the biological activity of the newly designed and synthesized series N-substituted 3,4-pyrroledicarboximides 2a–2p. The compounds 2a–2p were obtained in good yields by one-pot, three-component condensation of pyrrolo[3,4-c]pyrrole scaffold (1a–c) with secondary amines and an excess of formaldehyde solution in C2H5OH. The structural properties of the compounds were characterized by 1H NMR, 13C NMR FT-IR, MS, and elemental analysis. Moreover, single crystal X-ray diffraction has been recorded for compound 2h. The colorimetric inhibitor screening assay was used to obtain their potencies to inhibit COX-1 and COX-2 enzymes. According to the results, all of the tested compounds inhibited the activity of COX-1 and COX-2. Theoretical modeling was also applied to describe the binding properties of compounds towards COX-1 and COX-2 cyclooxygenase isoform. The data were supported by QSAR study.
Słowa kluczowe
pyrrolo[3, 4-c]pyrrole, cyclic imides, COX-1/COX-2 inhibition, Mannich bases, analgesic activity, inflammatory agents, docking study
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Pełny tekst licencji: https://creativecommons.org/licenses/by/3.0/pl/legalcode
Adres publiczny
http://dx.doi.org/10.3390/ijms22031410
Strona internetowa wydawcy
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