SYNTHESIS, EVALUATION OF ANALGESIC AND ANTI-INFLAMMATORY ACTIVITIES OF SUBSTITUTED 1,2-BENZOXAZOLONE AND 3-CHLORO-1,2-BENZOXAZOLE DERIVATIVESAbstract
Herein method for the synthesis of substituted 1,2-benzoxazolone (8a-f) and 3-chloro-1,2-benzoxazole (9a-f) derivatives has been described. A new scheme has been adapted for the construction of 1,2-benzoxazole ring from salicylic acid and its derivatives which leads to the formation of series of 5,6 and 7 substituted title compounds. Synthesized compounds were characterized by IR, 1H-NMR and Mass spectral analysis. Spectral data confirmed the compounds formation. Final compounds (8a-f) and (9a-f) were screened for their in-vivo analgesic activity by acetic acid induced writhing method in rats and anti-inflammatory activity by carrageenan-induced paw edema model. Among the compounds screened compound 8a and compound 9c showed good analgesic activity of about 45% (writhing mean 8.9) and 54% (writhing mean 7.5) inhibition respectively at 5 mg/Kg po dosage. Compounds 8b and 9b (both having inhibition edema of 66.1%) showed significant anti-inflammatory activity. Other derivatives exhibit moderate to good analgesic and anti-inflammatory activities.
B. Ravi Kiran , G. R. Vijayakumar * H. S. Bharath , R. Sivakumar , S. Sindhu and M. Shet Prakash
Department of Chemistry , University College of Science, Tumkur University, Tumkur, Karnataka, India
12 November, 2014
02 February, 2015
18 March, 2015
01 July, 2015