Anti-inflammatory activity of 3-thiazolyl coumarins. | [Journal of Chemical Society of Pakistan • 2017]

Author(s):

1. Uzma Salar: H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi,Pakistan

2. Khalid Mohammed Khan: H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Pakistan.

3. Almas Jabeen: Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Pakistan.

4. Aisha Faheem: Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Pakistan.

5. Muhammad Taha: Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, Dammam, Saudi Arabia.

6. Farman Ali: H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi,Pakistan

7. Shazia Syed: H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi,Pakistan

8. Syed Moazzam Haider: H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Pakistan

9. Shahnaz Perveen: PCSIR Laboratories Complex, Karachi, Shahrah-e-Dr. Salimuzzaman Siddiqui, Karachi, Pakistan.

10. 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.

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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