Synthesis of Highly Potent Anti-Inflammatory Compounds (ROS Inhibitors) from Isonicotinic Acid
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 <b>5</b>–<b>6&...
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MDPI AG
2021-02-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/5/1272 |
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| author | Sana Yaqoob Nourina Nasim Rahila Khanam Yan Wang Almas Jabeen Urooj Qureshi Zaheer Ul-Haq Hesham R. El-Seedi Zi-Hua Jiang Farooq-Ahmad Khan |
| author_facet | Sana Yaqoob Nourina Nasim Rahila Khanam Yan Wang Almas Jabeen Urooj Qureshi Zaheer Ul-Haq Hesham R. El-Seedi Zi-Hua Jiang Farooq-Ahmad Khan |
| author_sort | Sana Yaqoob |
| collection | DOAJ |
| description | 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 <b>5</b>–<b>6</b> and <b>8a</b>–<b>8b</b>. The compound <b>5</b> exhibits an exceptional IC<sub>50</sub> 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. |
| first_indexed | 2024-03-09T00:29:45Z |
| format | Article |
| id | doaj.art-bca56bec759e40db8d53012b1af7685f |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-09T00:29:45Z |
| publishDate | 2021-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-bca56bec759e40db8d53012b1af7685f2023-12-11T18:36:32ZengMDPI AGMolecules1420-30492021-02-01265127210.3390/molecules26051272Synthesis of Highly Potent Anti-Inflammatory Compounds (ROS Inhibitors) from Isonicotinic AcidSana Yaqoob0Nourina Nasim1Rahila Khanam2Yan Wang3Almas Jabeen4Urooj Qureshi5Zaheer Ul-Haq6Hesham R. El-Seedi7Zi-Hua Jiang8Farooq-Ahmad Khan9Third World Center for Science and Technology, H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, PakistanThird World Center for Science and Technology, H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, PakistanThird World Center for Science and Technology, H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, PakistanThird World Center for Science and Technology, H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, PakistanDr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, PakistanThird World Center for Science and Technology, H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, PakistanThird World Center for Science and Technology, H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, PakistanInternational Research Center for Food Nutrition and Safety, Jiangsu University, Zhenjiang 212013, ChinaDepartment of Chemistry, Lakehead University, 955 Oliver Road, Thunder Bay, ON P7B 5E1, CanadaThird World Center for Science and Technology, H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, PakistanIn 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 <b>5</b>–<b>6</b> and <b>8a</b>–<b>8b</b>. The compound <b>5</b> exhibits an exceptional IC<sub>50</sub> 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.https://www.mdpi.com/1420-3049/26/5/1272anti-inflammatoryROS inhibitorsisonicotinic acidpyridine carboxylic acidmolecular docking studies |
| spellingShingle | Sana Yaqoob Nourina Nasim Rahila Khanam Yan Wang Almas Jabeen Urooj Qureshi Zaheer Ul-Haq Hesham R. El-Seedi Zi-Hua Jiang Farooq-Ahmad Khan Synthesis of Highly Potent Anti-Inflammatory Compounds (ROS Inhibitors) from Isonicotinic Acid Molecules anti-inflammatory ROS inhibitors isonicotinic acid pyridine carboxylic acid molecular docking studies |
| title | Synthesis of Highly Potent Anti-Inflammatory Compounds (ROS Inhibitors) from Isonicotinic Acid |
| title_full | Synthesis of Highly Potent Anti-Inflammatory Compounds (ROS Inhibitors) from Isonicotinic Acid |
| title_fullStr | Synthesis of Highly Potent Anti-Inflammatory Compounds (ROS Inhibitors) from Isonicotinic Acid |
| title_full_unstemmed | Synthesis of Highly Potent Anti-Inflammatory Compounds (ROS Inhibitors) from Isonicotinic Acid |
| title_short | Synthesis of Highly Potent Anti-Inflammatory Compounds (ROS Inhibitors) from Isonicotinic Acid |
| title_sort | synthesis of highly potent anti inflammatory compounds ros inhibitors from isonicotinic acid |
| topic | anti-inflammatory ROS inhibitors isonicotinic acid pyridine carboxylic acid molecular docking studies |
| url | https://www.mdpi.com/1420-3049/26/5/1272 |
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