In silico screening, synthesis, in vitro evaluations antibacterial and DPPH scavenging activity of some 1,3,5-trisubstituted 2-pyrazoline derivatives as dihydrofolate reductase inhibitors

• Authors: S. Suriya , V. Mala
• Languages of publication: EN

Abstracts

EN

In this work, synthesis of three pyrazoline derivatives (6-8) is described. (E)-1,3-(phenylsubstituted)-prop-2-en-1-one (3-5) is prepared by the reaction of substituted benzaldehyde with 4-methylacetophenone, whereas condensation cyclization of the same chalcones (3-5) with phenylhydrazine hydrate in ethanol yielded 6-8. The structures of the title compounds (6-8) were characterized by chemical reactions, elemental analysis, and spectral methods such as IR spectra. The synthesized chalcone and pyrazolines were evaluated for in-vitro antibacterial and antioxidant activities against standard. The zone of inhibition for some of the newly synthesized compounds showed notable antibacterial activity against selected bacterial strains when compared with ampicillin. Significant antioxidant activities were also shown by chalcone and pyrazolines.

Keywords

EN

Synthesis; antibacterial; antioxidant; chalcone; pyrazoline

Discipline

• BIOCHEMISTRY: BIOCHEMISTRY

• Publisher: Scientific Publishing House „DARWIN”
• Journal: World News of Natural Sciences
• Year: 2018
• Volume: 18
• Issue: 2
• Pages: 180-186

Contributors

author

S. Suriya

• Department of Chemistry, Annai College of Arts and Science, Kovilacheri, Kumbakonam, Tamil Nadu - 612 503, India

author

V. Mala

• Department of Chemistry, Annai College of Arts and Science, Kovilacheri, Kumbakonam, Tamil Nadu - 612 503, India

References

• [1] Bano, S.; Javed, K.; Ahmad, S.; Rathish, L.G.; Singh, S.; Alam, M. S. Eur. J. Med. Chem. 2011, 46, 5763.
• [2] Bai, X.; Shi, W. Q.; Chen, H. F.; Zhang, P.; Li, Y.; Yin, S. F. Chem. Nat. Compd. 2012, 48, 60.
• [3] Lee, M.; Brockway, O.; Dandavati, A.; Tzou, S.; Sjoholm, R.; Satam, V.; Westbrook, C.; Mooberry, S. L.; Zeller, M.; Babu, B.; Lee, M. Eur. J. Med. Chem. 2011, 46, 3099.
• [4] Tandon, V. K.; Yadav, D. B.; Chaturvedi, A. K.; Shukla, P. K. Bioorg. Med. Chem. Lett. 2005, 15, 3288.
• [5] Akbas, E.; Berber, I. Eur. J. Med. Chem. 2005, 40, 401.
• [6] Bekhit, A. A.; Ashour, H. M. A.; Ghany, Y. S. A.; Bekhit, A. E. A.; Baraka, A. Eur. J. Med. Chem. 2008, 43, 456.
• [7] Penning, T. D.; Talley, J. J.; Bertenshaw, S. R.; Carter, J. S.; Collins, P. W.; Docter, J. Med. Chem. 1997, 40, 1347.
• [8] Deng, X.; Mani, N. S. Org. Lett. 2008, 10, 1307.
• [9] Katritzky, A. R.; Wang, M.; Zhang, S.; Voronkov, M. V. J. Org. Chem. 2001, 66, 6787.
• [10] Deng, X.; Mani, N. S. Org. Lett. 2006, 8, 3505
• [11] Senbagam, M. Rajarajan, R. Vijayakumar, V. Manikandan, S. Balaji, Vanangamudi, G. Thirunarayanan, World Scientific News 8 (2015) 211-226
• [12] Thirunarayanan, V. Sathiyendiran, R. Arulkumarn, R. Sundararrajan, Manikandan, G. Vanangamudi, World Scientific News 9 (2015) 46-69
• [13] P. Christuraj, P. R. Rajakumar, C. Geetha, G. Vanangamudi, R. Arulkumran, V. Manikandan, R. Sundararajan, G. Thirunarayanan, World Scientific News 74 (2017) 15-35
• [14] G. Thirunarayanan, N. Dinesh Kumar, World Scientific News 74 (2017) 251-266
• [15] P. W. Kibaba, H. Louis, K. K. Kering, V. N. Matiru. World Scientific News 74 (2017) 238-250
• [16] YK. Kang, K. Shin, KH. Yoo, KJ. Seo, CY. Hong, CS. Lee, SY. Park, DJ. Kim, SW. Park . Bioorg Med Chem Lett. 2000; 10: 95–9.
• [17] M. Rowley, HB. Broughton, I. Collins, R. Baker, F. Emms, R. Marwood, S. Patel, CI. Ragan. J Med Chem. 1996; 39: 1943-1945.
• [18] K. Kato, S. Terao, N. Shimamoto and M. Hirata, Studies on Scavengers of Active Oxygen Species. 1. Synthesis and Biological Activity of 2-O Alkylascorbic Acids, Journal of Medicinal Chemistry, Vol. 31, No. 4, 1988, pp. 793-798. doi:10.1021/jm00399a019

• Document Type: article