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Vol. 1 No. 4 (2010): October-December 2010

Synthesis, Anti-bacterial, Analgesic and Anti-inflammatory Activities of Some New Biologically Important Indazole Derivatives

DOI
https://doi.org/10.37285/ijddd.1.4.5
Submitted
November 25, 2024
Published
2024-11-28

Abstract

A series of new indazolyl derivatives (1.1A - 1.5E) have been prepared from commercially available N-methyl-3-indazole carboxylic acid and 7-amino cephalosporic acid. The synthesized compounds were evaluated for anti-bacterial, analgesic and in vivo anti-inflammatory activities using acetic acid writhing in mice and carrageenan paw oedema method in mice. The series of compounds have analgesic activity in the order 1.4D>1.3C>1.5E>1.2B >1.1A Compound 1.3C had maximum zone of inhibition for Bacillus thurengensis, Staphylococus aureus, Bacillus Subtilis and showed least zone of inhibition to E. coli. It did not show any zone of inhibition to remaining bacteria. Compound 1.2B showed maximum zone of inhibition to Bacillus thurengensis and E. coli. Compound 1.1A showed maximum zone of inhibition Proteus vulgaris Bacillus Subtilis and Bacillus thurengensis

References

  1. [1] Elguero, J. In Comprehensive Heterocyclic Chemistry II; Katritaky, A. R., Rees, C. W.,Scriven, E. F., Eds.; Elsevier: Oxford, 1996; Vol. 3, pp1–75.
  2. [2] Mahajan, R. N.; Havaldar, F. H.; Fernandes, P. S.J. Indian Chem. Soc. 1991, 68, 245.
  3. [3] (a) Genin, M. J.; Biles, C.; Keiser, B. J.; Poppe, S. M.;Swaney, S. M.; Tarpley, W. G.; Yagi, Y.; Romero, D. L.J. Med. Chem. 2000, 43, 1034
  4. [4] (a) Badawey, E.; El-Ashmawey, I. M. Eur. J. Med. Chem.1998, 33, 349; (b) Sui, Z.; Guan, J.; Ferro, M. P.; McCoy,K.; Wachter, M. P.; Murray, W. V.; Singer, M.; Steber,M.; Ritchie, D. M.; Argentieri, D. C. Bio-org. Med. Chem.Lett. 2000, 10, 601.
  5. [5] Bailey, D. M.; Hansen, P. E.; Hlavac, A. G.; Baizman,
  6. E. R.; Pearl, J.; Defelice, A. F.; Feigenson, M. E. J. Med.Chem. 1985, 28, 256.
  7. [6] Kees, K. L.; Fitzgerald, J. J.; Steiner, K. E.; Mattes, J. F.;Mihan, B.; Tosi, T.; Mondoro, D.; McCaleb, M. L.J. Med. Chem. 1996, 39, 3920.
  8. [7] Lyga, J. W.; Patera, R. M.; Plummer, M. J.; Halling, B. P.;Yuhas, D. A. Pestic. Sci. 1994, 42, 29.8. Xie, W.; Chipman, J.; Robertson, D. L.; Erikson, R. L.;Simmons,D. L. Proc. Natl. Acad. Sci. U.S.A. 1991, 88,2692–2696.
  9. [8] Xie, W.; Chipman, J.; Robertson, D. L.; Erikson, R. L.;Simmons, D. L. Proc. Natl. Acad. Sci. U.S.A. 1991, 88,2692–2696.
  10. [9] (a) Vane, J. R.; Botting, R. M. Inflammation Res. 1998,47,S78–S87; (b) Katori, M.; Majima, M.; Harada, Y.Inflammation Res. 1998, 47, S107–S111.
  11. [10] (a) Southgate R.Contemp.Org.Synth 1, 417, 1994.
  12. (b) Morin R B, Gorman, M. Chemistry and Biology of β-Lactam Antibiotics; Academic
  13. [11] Mata E G, Fraga M A, Delpiccolo C M L. J. Comb. Chem.5, 208, 2003.
  14. [12] Staudinger H. Liebigs Ann. Chem. 356, 61, 1907.
  15. [13] Clark H T, Johnson J R, Robinson R. The Chemistry of Penicillin, Princeton University Press: Princeton, NJ, 1949.
  16. [14] Page E I. The Chemistry of β-Lactase, Blackie Academic and Professional: New York, 1992.
  17. [15] (a) Niccolai D, Trasi L, Thomas R. J. Chem.Commun.2233, 1997.(b) Chu D T W, Ptattner J I, Katz L. J. Med. Chem. 39 3853, 1996.
  18. [16] Van der Steen F H, Van Koten, G. Tetrahedron 47, 7503 1991.

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