Synthesis of Highly Potent Anti-Inflammatory Compounds (ROS Inhibitors) from Isonicotinic Acid.
Molecules
; 26(5)2021 Feb 26.
Article
en En
| MEDLINE
| ID: mdl-33652837
ABSTRACT
In search of anti-inflammatory compounds, novel scaffolds containing isonicotinoyl motif were synthesized via an efficient strategy. The compounds were screened for their in vitro anti-inflammatory activity. Remarkably high activities were observed for isonicotinates 5-6 and 8a-8b. The compound 5 exhibits an exceptional IC50 value (1.42 ± 0.1 µg/mL) with 95.9% inhibition at 25 µg/mL, which is eight folds better than the standard drug ibuprofen (11.2 ± 1.9 µg/mL). To gain an insight into the mode of action of anti-inflammatory compounds, molecular docking studies were also performed. Decisively, further development and fine tuning of these isonicotinates based scaffolds for the treatment of various aberrations is still a wide-open field of research.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Antiinflamatorios no Esteroideos
/
Especies Reactivas de Oxígeno
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Inflamación
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Ácidos Isonicotínicos
Límite:
Humans
Idioma:
En
Año:
2021
Tipo del documento:
Article