Benzoxazole-Coumarin Derivatives: Potential Candidates for Development of Safer Anti-inflammatory Drugs

Many naturally existing antioxidants contain coumarin nucleus as a common pharmacophore whereas benzoxazole is identified as pharmacophore for anti-inflammatory activity from benoxaprofen, a potent anti-inflammatory drug. These two therapeutically important nuclie were coupled to generate two series of benzoxazole-coumarin derivatives (4a-4e and 5a-5e) for the development of novel compounds having potent anti-inflammatory and antioxidant activities with insignificant or no ulcerogenic potential. All compounds were evaluated for antioxidant, anti-inflammatory, ulcerogenic potential and oxidative stress induction. Compound 5e has been found to be the most potent antioxidant among these and in comparison to standard drug, BHT. Anti-inflammatory activity evaluation though in vitro hRBC method and in vivo rat paw edema model revealed that 5c exhibits maximum inhibition of hRBC lysis (92.5%) and inhibition of paw edema (52.7%). Results of in vivo biochemical estimations and evaluation of ulcerogenic potential shows that 5c is maximally safe to gastric mucosa. It is also proposed to cause no phototoxicity owing to radical scavenging ability of coumarin nucleus in it. Findings of the present study revealed that compound 5c may be taken as lead benzoxazole-coumarin derivative for development of safe anti-inflammatory agents.

Author(s): Richa Minhas, Sonali Sandhu, Yogita Bansal, Gulshan Bansal

Abstract | Full-Text | PDF

Share This Article