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- Title
Anti-inflammatory Activity of 3-Thiazolyl Coumarins.
- Authors
Salar, Uzma; Khan, Khalid Mohammed; Jabeen, Almas; Bakhtawar; Faheem, Aisha; Taha, Muhammad; Ali, Farman; Syed, Shazia; Kanwal; Haider, Syed Moazzam; Perveen, Shahnaz
- Abstract
3-Thiazolyl coumarins 1-33 along with coumarin scaffold (IC50 = 5.2 ± 0.2 µg/mL) were evaluated for in vitro antiinflammatory activity. Activity of compounds was investigated by looking their influence on oxidative burst activity of zymosan stimulated whole blood phagocytes by using a luminol enhanced chemiluminescence technique. Ibuprofen was used as standard drug (IC50 = 54.2 ± 9.2 µM). Four 3-thiazolyl coumarin derivatives 9 (IC50 = 31.0 ± 2.5 µg/mL), 13 (IC50 = 27.1 ± 4.2 µg/mL), 18 (IC50 = 5.6 ± 2.6 µg/mL), and 29 (IC50 = 1.9 ± 1.0 µg/mL) out of thirty-three demonstrated antiinflammatory activity as compared to the standard ibuprofen (IC50 = 11.2 ± 1.9 µg/mL). Especially, compound 29 showed many folds better activity as compared to coumarin and standard ibuprofen. Structure-activity relationship was also established. It is worth-mentioning that active analogs 9, 13, 18, and 29 were found to be non-toxic on NIH-3T3 mouse fibroblast cell line.
- Subjects
ANTI-inflammatory agents; COUMARINS; ZYMOSAN; PHAGOCYTES; CHEMILUMINESCENCE
- Publication
Journal of the Chemical Society of Pakistan, 2017, Vol 39, Issue 4, p578
- ISSN
0253-5106
- Publication type
Article