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Anti-inflammatory activity of 3-thiazolyl coumarins.
Author(s)
Uzma Salar H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi,Pakistan
Khalid Mohammed Khan H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Pakistan.
Almas Jabeen Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Pakistan.
Aisha Faheem Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Pakistan.
Muhammad Taha Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, Dammam, Saudi Arabia.
Farman Ali H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi,Pakistan
Shazia Syed H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi,Pakistan
Syed Moazzam Haider H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Pakistan
Shahnaz Perveen PCSIR Laboratories Complex, Karachi, Shahrah-e-Dr. Salimuzzaman Siddiqui, Karachi, Pakistan.
Bakhtawar H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan
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.
Publication Details
Page(s) 578-585
DOI DOI not available
Published Journal: Journal of Chemical Society of Pakistan, Volume: 39, Issue: 4, Year: 2017
Keywords
ibuprofen synthesis nontoxic antiinflammatory activity coumarin
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