EVALUATION AND STUDIES ON THE STRUCTURAL IMPACT OF SUBSTITUTED 4, 5-DIHYDROISOXAZOLES ON THEIR BIOLOGICAL ACTIVITIES
Abstract
In present study, a series of isoxazole derivatives synthesized were evaluated for antimicrobial activities by disc diffusion method. Some compounds of the series exhibited promising antibacterial and antifungal activity compared to standard drugs. The minimum inhibitory concentration (MIC’s) was determined against each organism. The compounds were tested for their in-vitro antioxidant activity and reducing power ability. Free radicals play an important role in various pathological and xenotoxic effects so antioxidant may have protective role in these pathological conditions. Based on the results of an antimicrobial, anti-oxidant study, the effect of substitution on the activity and possible structure activity relationship of the compounds for their antioxidant activity is presented.
Keywords:
Isoxazoles, antibacterial, antifungal, antioxidant, reducing powerDOI
https://doi.org/10.25004/IJPSDR.2012.040403References
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14. Panda SS, Chowdary PVR, Jayashree BS. Synthesis, Anti inflammatory and antibacterial activity of novel Indolyl-isoxazoles. Ind J Pharm Sci 2009; 71:684-687.
15. Jayaroopa P, Vasanth Kumar G, Renuka N, Ajay Kumar K. Synthesis of new 3,5-diaryl-4,5-dihydroisoxazole-4-carbonitriles via 1,3-dipolar cycloaddition. IOSR J App Chem. 2012; 1(4):20-23.
16. Vasanth Kumar G, Govindaraju M, Renuka N, Bi Bi Ahmadi Khatoon, Mylarappa BN, Ajay Kumar K. Synthesis of 1,3,5-triaryl-4,6-dioxo-pyrrolo[3,4-d]-7,8-dihydropyrzoles and their antimicrobial and antioxidant activity. Rasayan J Chemistry. 2012; 5(3): 338-342.
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18. Ajay Kumar K, Lokanatha Rai KM, Vasanth Kumar G, Mylarappa BN. A facile route for the synthesis of ethyl N-aryl-2, 6-dioxo-piperid-3-ene-4-carboxylates and their biological activity. Int J Pharm Pharm Sci. 2012; 4(Suppl 4):564-568.
19. Govindaraju M, Vasanth Kumar G, Pavithra G, Harish Nayaka MA, Mylarappa BN, Ajay Kumar K. Evaluation of new tetra substituted pyrazolines for their antimicrobial and antioxidant activity; Structure-activity relationship, IOSR J Pharm Biolog Sci. 2012; 2(6):30-34.
2. Yildrim A, Oktay M, Bilaloǧlu V. The antioxidant activity of leaves of Cydonia vulgaris. Tur J Med Sci. 2001; 31:23-27.
3. Huang DH, Chen C, Lin C, Lin Y. Antioxidant and antiproliferative activities of water spinach (Ipomoea aquatica Forsk.) constituents. Bot Bull Acad Sci. 2005; 46:99-106.
4. Sun J, Chen Y, Li M, Ge Z. Role of antioxidant enzymes on ionizing radiation resistance. Free Radical Biology and Med. 1998; 42:586-592.
5. Khilfi S, Hachimi E, Khalil A, Es-Safi A, Belahyam A, Tellal A, El Abbouyi A. In-vitro antioxidant properties of Salvia verbenaca. L. hydromethanolic extract. Indian J Pharmacology. 2006; 38:276-280.
6. Gulcin I, Alici HA, Cesur M. Determination of in- vitro antioxidant and radical scavenging activities of propofol. Pharm Bull. 2005; 53:281-285.
7. Padmanabhan P, Jangle SN. Evaluation of DPPH radical scavenging activity and reducing power of four selected medicinal plants and their combinations. Int J Pharm Sci and Drug Res. 2012; (4)2:143-146.
8. Anjan Kumar, Sradhasini Rout, Panda CS, Raju MBV, Ravikumar BVV. Synthesis and biological evaluation of 3,5-diarylisoxazoles as antibacterial, antifungal and anti-inflammatory agents. J Adv Pharm Res. 2011; 2(2):94-101.
9. Ajay Kumar K, Govindaraju M, Vasantha Kumar G. Synthesis of isoxazoles via 1,3-dipolar cycloaddition reactions and their antimicrobial activity. Ind J Heterocycl Chem. 2010; 20:183-184.
10. Ajay Kumar K, Lokanatha Rai KM, Umesha KB. Synthesis and evaluation of antifungal and antibacterial activity of ethyl 3,5-diarylisoxazole-4-carboxylates. J Chem Res (S). 2001; 436-438.
11. Kamal A, Reddy JS, Ramaiah MJ, Dastagiri D, Bharathi EV, Azhar MA, Sultana F, Pushpavalli SNCVL, Bhadra MP, Juvekar A, Sen S, Zingde S. Design, synthesis and biological evaluation of 3,5-diaryl-isoxazoline/isoxazolepyrrolobenzodiazepine conjugates as potential anticancer agents. Eur J Med Chem. 2010; 45:3924-3937.
12. Changtam C, Hongmanee P, Suksamrarn A. Isoxazole analogs of curcuminoids with highly potent multidrug-resistant antimycobacterial activity. Eur J Med Chem. 2010, 45, 4446-4457.
13. Abdu Musad E, Mohamed R, Saeed BA, Vishwanath BS, Rai KML. Synthesis and evaluation of antioxidant and antibacterial activities of new substituted bis(1,3,4-oxadiazoles), 3,5-bis(substituted) pyrazoles and isoxazoles. Bioorg Med Chem Letters. 2011; 21(12):3536-3540.
14. Panda SS, Chowdary PVR, Jayashree BS. Synthesis, Anti inflammatory and antibacterial activity of novel Indolyl-isoxazoles. Ind J Pharm Sci 2009; 71:684-687.
15. Jayaroopa P, Vasanth Kumar G, Renuka N, Ajay Kumar K. Synthesis of new 3,5-diaryl-4,5-dihydroisoxazole-4-carbonitriles via 1,3-dipolar cycloaddition. IOSR J App Chem. 2012; 1(4):20-23.
16. Vasanth Kumar G, Govindaraju M, Renuka N, Bi Bi Ahmadi Khatoon, Mylarappa BN, Ajay Kumar K. Synthesis of 1,3,5-triaryl-4,6-dioxo-pyrrolo[3,4-d]-7,8-dihydropyrzoles and their antimicrobial and antioxidant activity. Rasayan J Chemistry. 2012; 5(3): 338-342.
17. Ajay Kumar K, Lokanatha Rai KM, Umesha KB. Evaluation of antibacterial activity of 3,5-dicyano-4,6-diaryl-4-ethoxycarbonyl-piperid-2-ones. J Pharma Biomed Anal. 2002; 27:837-840.
18. Ajay Kumar K, Lokanatha Rai KM, Vasanth Kumar G, Mylarappa BN. A facile route for the synthesis of ethyl N-aryl-2, 6-dioxo-piperid-3-ene-4-carboxylates and their biological activity. Int J Pharm Pharm Sci. 2012; 4(Suppl 4):564-568.
19. Govindaraju M, Vasanth Kumar G, Pavithra G, Harish Nayaka MA, Mylarappa BN, Ajay Kumar K. Evaluation of new tetra substituted pyrazolines for their antimicrobial and antioxidant activity; Structure-activity relationship, IOSR J Pharm Biolog Sci. 2012; 2(6):30-34.
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01-10-2012
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“EVALUATION AND STUDIES ON THE STRUCTURAL IMPACT OF SUBSTITUTED 4, 5-DIHYDROISOXAZOLES ON THEIR BIOLOGICAL ACTIVITIES”. International Journal of Pharmaceutical Sciences and Drug Research, vol. 4, no. 3, Oct. 2012, pp. 236-9, https://doi.org/10.25004/IJPSDR.2012.040403.
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How to Cite
“EVALUATION AND STUDIES ON THE STRUCTURAL IMPACT OF SUBSTITUTED 4, 5-DIHYDROISOXAZOLES ON THEIR BIOLOGICAL ACTIVITIES”. International Journal of Pharmaceutical Sciences and Drug Research, vol. 4, no. 3, Oct. 2012, pp. 236-9, https://doi.org/10.25004/IJPSDR.2012.040403.
