SYNTHESIS OF NEW DICLOFENAC DERIVATIVES BY COUPLING WITH CHALCONE DERIVATIVES AS POSSIBLE MUTUAL PRODRUGS

SYNTHESIS OF NEW DICLOFENAC DERIVATIVES BY COUPLING WITH CHALCONE DERIVATIVES AS POSSIBLE MUTUAL PRODRUGS
تحميل
بحث	النوع:
صيدلة	التخصص العام:
SAMER A. HASAN	اسم الناشر:
AMER N. ELIAS	اسماء المساعدين:
International Journal of Pharmacy and Pharmaceutical Sciences	الجهة الناشرة:
International Journal of Pharmacy and Pharmaceutical Sciences (Int J Pharm Pharm Sci) is peer-reviewed, monthly (Onward April 2014) open access Journal. IJPPS publishes original research work that contributes significantly to advance the scientific knowledge in pharmacy and pharmaceutical sciences including Pharmaceutical Technology, Pharmaceutics, Novel Drug Delivery, Biopharmaceutics, Pharmacokinetics Pharmacognosy and Natural Product Research Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmaceutical Analysis Pharmacology, Pharmacy Practice, Clinical and Hospital Pharmacy Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics, Pharmacoeconomics Research outcomes from medical sciences/case study and biotechnology of pharmaceutical interest are also considered.
2014	سنة النشر:
الخلاصة ABSTRACT Objectives: To synthesize a diclofenac-chalcones derivatives that can act as possible mutual prodrugs of enhanced anti-inflammatory activity and devoid of ulcerogenic side effects. Methods: Mutual prodrugs were synthesized by conjugation of Diclofenac with a series of eight chalcone derivatives by the Claisen–Schmidt condensation of acetophenone or p-hydroxyacetophenone with benzaldehyde or appropriately substituted benzaldehyde in the presence of SOCl2/EtOH as a catalyst. Results: The structure of the synthesized derivatives has been characterized by elemental microanalysis (CHN), FTIR Spectroscopy, and other physicochemical properties. The anti-inflammatory activity of the synthesized fluorinated chalcone derivative was performed using the cotton pellet-induced granuloma in rats as a model, and found to be comparable to dexamethasone in this regard. Conclusion: Chalcones with their pronounced anti-inflammatory activity can synergize the activity of Diclofenac when conjugated with this NSAID.