Pharmaceutical Chemistry Journal

, Volume 46, Issue 2, pp 117–121 | Cite as

Thiopyrimidine derivatives: synthesis and antibacterial activity

  • S. Baluja
  • N. Kacchadia
  • S. Chanda

Eleven thiopyrimidine derivatives have been synthesized and their antibacterial activity has been studied against four Gram positive (Bacillus cereus ATCC11778, Staphylococcus aureus ATCC29737, Staphylococcus epidermidids NCIM2493, and Micrococcus luteus ATCC10240) and three Gram negative (Proteus mirabilis NCIM2241, Escherichia coli ATCC25922, and Klebsiella aerogenes NICM2098) bacteria. The antibacterial activity was evaluated using the agar well diffusion method. The thiopyrimidine derivatives showed various activity against different bacterial strains, depending on their structural formula. Gram positive bacteria were more susceptible than Gram negative bacteria; E. coli was the most resistant, and B. cereus was the most susceptible bacteria. A thiopyrimidine derivative with methoxy group at the para position showed the best antibacterial activity, while the substitution of chloro, bromo, and methyl groups decreased the activity.

Key words

Thiopyrimidine derivatives antibacterial activity Gram positive bacteria Gram negative bacteria E. coli B. cereus 


  1. 1.
    S. Prachayasittikul, A. Worachartcheewan, C. Nantasenamat, M. Chinworrungsee, N. Sornsongkhram, S. Ruchirawat, and V. Prachayasittikul, Eur. J. Med. Chem., 46(2), 738 (2011).PubMedCrossRefGoogle Scholar
  2. 2.
    W. H. Usama, A. Mohamed Al-Omar, G. E. Abdel, and A. G. Amr, Arab. J. Chem., (2010), doi: 10.1016/j.arabjc.2010.09.019.
  3. 3.
    D. Bartaria, V. P. Shukla, and V. Krishna, J. Ind. Chem. Soc., 86, 9 (2009).Google Scholar
  4. 4.
    A. G. Amr, World J. Chem., 4(2), 201 (2009).Google Scholar
  5. 5.
    A. G. Amr, S. S. Maigali, and M. M. Abdulla, Monatsh. Chem. 139, 1409 (2008).CrossRefGoogle Scholar
  6. 6.
    S. Maddila and S. B. Jonnalagadda, Arch. Pharm. Chem. Life Sci., 000, 1 (2011).Google Scholar
  7. 7.
    P. Kamalakannan and D. Venkappayya, Russ. J. Coord. Chem., 28, 423 (2002).CrossRefGoogle Scholar
  8. 8.
    M. K. Jani, B. R. Shah and N. K. Udavia; Chem. Environ. Res., 1, 345 (1992).Google Scholar
  9. 9.
    M. Okabe, R. C. Sun, and G. Zenchoff; J. Org. Chem., 56, 4393 (1991).CrossRefGoogle Scholar
  10. 10.
    S. Sarangam and S. Somshekara; J. Ind. Chem. Soc., 53, 185 (1976).Google Scholar
  11. 11.
    Z. Machan and V. Krystyna; Acta. Pol. Chem. B, 42, 516 (1985).Google Scholar
  12. 12.
    R. P. Verma, S. M. Sondhi, N. Singhal, V. K. Sharma, R. Shukla, and G. K. Patnaik, Phosphorous, Sulfur, Silicon Relat. Elem., 118, 7 (1996).CrossRefGoogle Scholar
  13. 13.
    V. J. Ram, N. M. Haqu, and P. Y. Guru; Eur. J. Med. Chem., 27, 851 (1992).CrossRefGoogle Scholar
  14. 14.
    M. Ali, A. G. Hamman, and S. F. Mohmad, J. Phosphorus Sulfur; 39, 24 (1988).Google Scholar
  15. 15.
    C. R. Petric, H. B. Cotton, and P. A. Me Kerman; J. Med. Chem., 28, 1010 (1988).CrossRefGoogle Scholar
  16. 16.
    C. Perez, M. Paul, and P. Bazerque, Acta Biol. Med. Exp., 15, 113 (1990).Google Scholar
  17. 17.
    J. Parekh, P. Inamdhar, R. Nair, S. Baluja, and S. Chanda, J. Serb. Chem. Soc., 70, 1155 (2005).CrossRefGoogle Scholar
  18. 18.
    A. Trilla and J. M. Miro, J Chemotherap., 7 (Suppl), 37 (1995).Google Scholar
  19. 19.
    A. D. M. Mathekga, J. J. M. Meyer, M. M. Horn and S. E. Drews, Phytochemistry 53, 93 (2000).PubMedCrossRefGoogle Scholar
  20. 20.
    J. P. O’Gara and H. Humphreys, J. Med. Microbiol., 50, 582 (2000).Google Scholar
  21. 21.
    M. Cheesbrough, Medical Laboratory Manual for Tropical Countries. Microbiology (Linacre House – Jordan Hill, Oxford, 2000), p. 260.Google Scholar
  22. 22.
    J. G. Black, Microbiology: Principles and Application (Prentice Hall, 1996), p. 260.Google Scholar
  23. 23.
    R. Nair, A. Shah, S. Baluja, and S. V. Chanda, Med. Chem. Res., 11, 463 (2002).Google Scholar
  24. 24.
    Y. Vaghsiya, R. Nair, M. Soni, S. Baluja, and S. Chanda, J. Serb. Chem. Soc., 69, 991 (2004).CrossRefGoogle Scholar

Copyright information

© Springer Science+Business Media, Inc. 2012

Authors and Affiliations

  1. 1.Physical Chemistry Laboratory, Department of ChemistrySaurashtra UniversityRajkotIndia
  2. 2.Phytochemical, Pharmacological and Microbiological Laboratory, Department of BiosciencesSaurashtra UniversityRajkotIndia

Personalised recommendations