4972-66-1Relevant academic research and scientific papers
Synthesis of highly potent anti-inflammatory compounds (ROS inhibitors) from isonicotinic acid
Yaqoob, Sana,Nasim, Nourina,Khanam, Rahila,Wang, Yan,Jabeen, Almas,Qureshi, Urooj,Ul-Haq, Zaheer,El-Seedi, Hesham R.,Jiang, Zi-Hua,Khan, Farooq-Ahmad
, (2021)
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 antiinflammatory 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.
