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2018 | 18 | 2 |

Tytuł artykułu

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

Autorzy

Treść / Zawartość

Warianty tytułu

Języki publikacji

EN

Abstrakty

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.

Słowa kluczowe

Wydawca

-

Rocznik

Tom

18

Numer

2

Opis fizyczny

p.180-186,fig.,ref.

Twórcy

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

Bibliografia

  • [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

Typ dokumentu

Bibliografia

Identyfikatory

Identyfikator YADDA

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