SYNTHESIS AND EVALUATION OF ANTI-INFLAMMATORY AND ANTIBACTERIAL ACTIVITIES OF SOME 1, 2-BENZISOXAZOLE DERIVATIVES
Abstract
Objective: A series of 1, 2-Benzisoxazole derivatives were synthesized and characterized by various analytical techniques like Melting point, Rf, FTIR, and NMR spectra.
Methods: Structures of the compounds were elucidated and evaluated for anti-inflammatory activity by HRBC membrane stabilization method, antibacterial activity against Escherichia coli and Staphylococcus aureus by cup plate method.
Results: The compounds 4a and 4e showed good anti-inflammatory activity compared with standard drug Diclofenac sodium and compounds 4b and 4d showed good antibacterial activity on compared with standard drug Gentamycin.
Conclusion: These compounds may serve as future leads for anti-inflammatory and antibacterial drug discovery.
Keywords:
1, 2-Benzisoxazole, Anti-inflammatory, Antibacterial activity
References
1. Robert L Findling, Michael G Aman, Marielle Eerdekens, Albert Derivan, Ben Lyons, Long-Term. Open-Label study of risperidone in children with severe disruptive behaviors and below-average IQ. Am J Psychiatry 2004;161:677-84.
2. Gaetano Zaccara, Luigi M Specchio. Long-term safety and effectiveness of zonisamide in the treatment of epilepsy: a review of the literature. Neuropsychiatr Dis Treat 2009;5:249–59.
3. Baulac M. The long-term retention of zonisamide in a large cohort of people with epilepsy at a tertiary referral center. Epilepsy Res 2006;2:S3–S9.
4. Veera Reddy Arava, Udaya Bhaskara Rao Siripalli, Vaishali Nadkarni, Rajendiran Chinnapillai. Novel base-catalyzed rearrangement of sultone oximes to 1, 2-benzisoxazole-3-methane sulfonate derivatives. Beilstein J Org Chem 2007;3:20.
5. K Madhavi, K Bharathi, KVSRG Prasad. Synthesis and evaluation of 3-methyl-4-nitro-5-(substituted styryl) isoxazoles for antioxidant and anti-inflammatory activities. Res J Pharm Biol Chem Sci 2010;1:1073-82.
6. Ravindra M Kumbhare, VN Ingle. Synthesis of novel benzothiazole and benzisoxazole functionalized unsymmetrical alkanes and study of their antimicrobial activity. Indian J Chem 2009;48:996-1000.
7. Vijay kumar Tirlapur, Narasimha Gandhi, Raga Baswaraj, Rajendra Prasad Y. Synthesis, characterization and biological activities of some pyrimidines and isoxazoles bearing benzofuran moiety. Int J ChemTech Res 2010;2:1434-40.
8. RA Shastri, JS Varudkar. Synthesis and antimicrobial activity of 3-propene 1, 2-benzisoxazole derivatives. Indian J Chem 2009;48B:1156-60.
9. Varadarasou Mouttaya Mounnissamy, Subrahmanyan Kavimani, Vaithilingam Balu, Sabarimuthu Darlin Quine. Evaluation of anti-inflammatory and membrane stabilizing properties of ethanol extract of Cansjera rheedii J. Gmelin (Opiliaceae). Iranian J Pharmacol Ther 2007;6:235-7.
10. G Prakash Yoganandam, K Ilango, Sucharita De. Evaluation of anti-inflammatory an membrane stabilizing properties of various extracts of Punica granatum L (Lytheraceae). Int J PharmTech Res 2010;2:1260-3.
2. Gaetano Zaccara, Luigi M Specchio. Long-term safety and effectiveness of zonisamide in the treatment of epilepsy: a review of the literature. Neuropsychiatr Dis Treat 2009;5:249–59.
3. Baulac M. The long-term retention of zonisamide in a large cohort of people with epilepsy at a tertiary referral center. Epilepsy Res 2006;2:S3–S9.
4. Veera Reddy Arava, Udaya Bhaskara Rao Siripalli, Vaishali Nadkarni, Rajendiran Chinnapillai. Novel base-catalyzed rearrangement of sultone oximes to 1, 2-benzisoxazole-3-methane sulfonate derivatives. Beilstein J Org Chem 2007;3:20.
5. K Madhavi, K Bharathi, KVSRG Prasad. Synthesis and evaluation of 3-methyl-4-nitro-5-(substituted styryl) isoxazoles for antioxidant and anti-inflammatory activities. Res J Pharm Biol Chem Sci 2010;1:1073-82.
6. Ravindra M Kumbhare, VN Ingle. Synthesis of novel benzothiazole and benzisoxazole functionalized unsymmetrical alkanes and study of their antimicrobial activity. Indian J Chem 2009;48:996-1000.
7. Vijay kumar Tirlapur, Narasimha Gandhi, Raga Baswaraj, Rajendra Prasad Y. Synthesis, characterization and biological activities of some pyrimidines and isoxazoles bearing benzofuran moiety. Int J ChemTech Res 2010;2:1434-40.
8. RA Shastri, JS Varudkar. Synthesis and antimicrobial activity of 3-propene 1, 2-benzisoxazole derivatives. Indian J Chem 2009;48B:1156-60.
9. Varadarasou Mouttaya Mounnissamy, Subrahmanyan Kavimani, Vaithilingam Balu, Sabarimuthu Darlin Quine. Evaluation of anti-inflammatory and membrane stabilizing properties of ethanol extract of Cansjera rheedii J. Gmelin (Opiliaceae). Iranian J Pharmacol Ther 2007;6:235-7.
10. G Prakash Yoganandam, K Ilango, Sucharita De. Evaluation of anti-inflammatory an membrane stabilizing properties of various extracts of Punica granatum L (Lytheraceae). Int J PharmTech Res 2010;2:1260-3.
Statistics
414 Views | 689 Downloads
Citations
How to Cite
Sasikumar, S., H. M., and A. T. “SYNTHESIS AND EVALUATION OF ANTI-INFLAMMATORY AND ANTIBACTERIAL ACTIVITIES OF SOME 1, 2-BENZISOXAZOLE DERIVATIVES”. International Journal of Current Pharmaceutical Research, Vol. 8, no. 4, Oct. 2016, pp. 64-67, doi:10.22159/ijcpr.2016v8i4.15281.
Issue
Section
Original Article(s)
