|
|
|
|
Anti-inflammatory activity of 3-thiazolyl coumarins
|
|
|
|
|
|
|
|
نویسنده
|
salar u. ,khan k.m. ,jabeen a. ,bakhtawar h. e. j. research institute of chemistry ,faheem a. ,taha m. ,ali f. ,syed s. ,kanwal h. e. j. research institute of chemistry ,haider s.m. ,perveen s.
|
|
منبع
|
journal of the chemical society of pakistan - 2017 - دوره : 39 - شماره : 4 - صفحه:578 -585
|
|
چکیده
|
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.
|
|
کلیدواژه
|
Antiinflammatory activity; Coumarin; Ibuprofen; Non-toxic; Synthesis; Thiazole
|
|
آدرس
|
h. e. j. research institute of chemistry,international center for chemical and biological sciences,university of karachi,karachi, Pakistan, h. e. j. research institute of chemistry,international center for chemical and biological sciences,university of karachi,karachi, Pakistan, h. e. j. research institute of chemistry,international center for chemical and biological sciences,university of karachi,karachi, Pakistan, international center for chemical and biological sciences,university of karachi,karachi, Pakistan, dr. panjwani center for molecular medicine and drug research,international center for chemical and biological sciences,university of karachi,karachi, Pakistan, department of clinical pharmacy,institute for research and medical consultations (irmc),university of dammam,dammam, Saudi Arabia, h. e. j. research institute of chemistry,international center for chemical and biological sciences,university of karachi,karachi, Pakistan, h. e. j. research institute of chemistry,international center for chemical and biological sciences,university of karachi,karachi, Pakistan, international center for chemical and biological sciences,university of karachi,karachi, Pakistan, h. e. j. research institute of chemistry,international center for chemical and biological sciences,university of karachi,karachi, Pakistan, pcsir laboratories complex,karachi,shahrah-e-dr. salimuzzaman siddiqui,karachi, Pakistan
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
Authors
|
salar ,khan ,jabeen ,bakhtawar ,faheem ,taha ,ali ,syed ,kanwal ,haider ,perveen
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|