Synthesis, Characterization, and Anti-inflammatory activity of Some Novel Oxazole Derivatives
A series of novel oxazole derivatives (A, A1, A2) were synthesized starting from acetone and urea. The compound (A) was obtained by heating it with acetophenone and urea in iodine. Compound (A) on treatment with 4-amino benzaldehyde (Z)-N-(4-amino benzylidine)-4-((E)-Penta-2, 4-diene-2) oxazole-2-amine afforded (A1). Acylation of compound (A) with 4-amino benzoyl chloride to obtain the corresponding N-(4 phenyl oxazole-2- yl)- benzamide (A2). The structures of compounds have been established employing FTIR and 1H-NMR spectral analysis. All oxazole derivatives were evaluated for anti-inflammatory activity by the carrageenan-induced Rat hind paw method. Derivative A1 shows maximum anti-inflammatory activity.
Keywords: Oxazoles, anti-inflammatory, Benzamide, acetophenone, indomethacin.
2. Ahmad H, Ullah S, Rahman F, Saeed A, Pelletier J, Sévigny J, et al. Synthesis of biphenyl oxazole derivatives via Suzuki coupling and biological evaluations as nucleotide pyrophosphatase/phosphodiesterase-1 and -3 inhibitors. Eur J Med Chem. 2020; 208. https://doi.org/10.1016/j.ejmech.2020.112759
3. Kaur R, Palta K, Kumar M, Bhargava M, Dahiya L. Therapeutic potential of oxazole scaffold: a patent review (2006–2017). Expert Opin Ther Pat [Internet]. 2018; 28(11):783–812. Available from: https://doi.org/10.1080/13543776.2018.1526280
4. Zhang HZ, Zhao ZL, Zhou CH. Recent advance in oxazole-based medicinal chemistry. Eur J Med Chem [Internet]. 2018; 144:444–92. Available from: https://doi.org/10.1016/j.ejmech.2017.12.044
5. Brunton LLJSLLP. Goodman and Gilman’s The Pharmacological Basis of Therapeutics. Vol. 11, JAMA: The Journal of the American Medical Association. 2002. 2052–2052 p. https://doi.org/10.1001/jama.288.16.2052
6. Ajay Kumar Garg*, Ranjan Kumar Singh , Khushboo Srimali , Saurabh K. Sinha VJ. semicarbazones as anticonvulsant molecules. Adv Pharm J. 2022; 7(1):1–6.
7. Shakya AK, Kaur A, Al-Najjar BO, Naik RR. Molecular modeling, synthesis, characterization and pharmacological evaluation of benzo[d]oxazole derivatives as non-steroidal anti-inflammatory agents. Saudi Pharm J [Internet]. 2016; 24(5):616–24. Available from: http://dx.doi.org/10.1016/j.jsps.2015.03.018
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