Synthesis and Antithyroid Activity of Some 8-Substituted Purine Derivatives

Authors

  • Ismat Fatima University of the Punjab
  • Munawar A. Munawar University of the Punjab
  • Affia Tasneem CENUM

Keywords:

8-sulfanyl-3,9-dihydro-1H-purine-2,6-dione; derivatives; antithyroid activity; thyroid hormones; histology.

Abstract

Some novel as well as known derivatives of 8-sulfanyl-3,9- dihydro-1H-purine-2,6 dione were synthesized and their antithyroid activity was measured in rats after administration of a daily dose of 20mg/kg via i.p. injection for 15 days. Free thyroxine and triiodothyronine concentrations were determined using radioimmunoassay technique. The assay results showed decrease in the hormonal concentrations for the animals treated with these compounds as compared to the control animals. Similarly, thyroid stimulating hormone level was measured with ELISA method and the results demonstrated a comparative increase of this hormone for the treated animals. The hormonal variations indicated significant (α≤0.05) activity of the compounds.

Histological study of thyroid tissues from the test animals showed cellular modifications in the treated animals like cylindrical shape of follicular epithelium, depletion of colloid and high values of thyroid body indices. All these factors further confirmed the antithyroid effects of the compounds under study.

Downloads

Download data is not yet available.

Author Biographies

Ismat Fatima, University of the Punjab

Institute of Chemistry

Munawar A. Munawar, University of the Punjab

Institute of Chemistry

Affia Tasneem, CENUM

Mayo Hospital

References

1. Trzepacz, P. T.; Klein, I.; Roberts, M.; Greenhouse, J.; Levey, G. S. Am. J. Med. 1989, 87, 558-561.
2. Cooper, D. S. Endo. Metab. Clin. North Am. 1998, 27, 225-247.
3. Raby, C.; Lagorce, J. F.; Jambut-Absil, A. C.; Buxeraud, J.; Catanzano, G., Endocrinol. 1990, 126, 1683-1691.
4. Buxeraud, J.; Jambut-Absil, A. C.; Raby, C. J. Pharm. Sci. 1984, 73, 1687-1690.
5. Bandyopadhyay, U.; Biswas, K.; Banerjee, R. K. Toxicol. Lett. 2002, 128, 117-127.
6. Jambut-Absil, A. C.; Buxeraud, J.; Claude, J.; Raby, C. Fr. Arzneimittel-Forschung 1987, 37, 772-777.
7. Abou-Shaaban Rafiq, R. A.; Al-Khamees, H. A.; Abou-Auda, H. S.; Simonelli, A. P. Saudi Pharm. J. 1995, 3, 156-175.
8. Dalton, M. E.; Pegg, A. E. Clin.Cancer. Res. 1997, 3, 837-847.
9. Hahn, H.; Boop, M. Biol. Unserer. Zeit. 1981, 11, 113-120.
10. Jacobson, K. A.; Van Galen, P. J. M.; Williams, M. J. Med. Chem. 1992, 35, 407-422.
11. Mann, F. G.; Porter, J. W. G. J. Chem. Soc. 1945, 751-760.
12. Fatima, I.; Munawar, M. A., Khan, M. A.; Sohail, N.; Amjad, R. Acta Cryst. 2009, E65, 02994.
13. Sariri, R.; Khalili, G. Russ. J. Org. Chem. 2002, 38, 1053-1055.
14. Loo, T. L.; Marvin, E.; Arthur, J.; Garceau, J.; Reid, C. J. Am.Chem. Soc. 1959, 81, 3039-3041.
15. Lagorce, J. F.; Comby, F.; Rousseau, A.; Buxeraud, J.; Raby, C. Chem. Pharm. Bull. 1993, 41, 1258-1260.
16. Shamsipur, M.; Mashhadizadeh, M. H. J. Inc. Phenom. Macrocycl. Chem. 2000, 38, 277-286.
17. Fatima, I.; Munawar, M. A.; Khan, M. A.; Asmatullah; Tasneem, A.; Khalil, M. J. Braz. Chem. Soc. 2010, 21, 1699-1703.
18. Bergmann, F.; Gorvin, H. K.; Waron, H. U.; Kalmus, A. Biochem, J. 1963, 86, 567-574.

Downloads

Published

2019-06-05

Issue

Vol. 54 No. 4 (2010): Regular Issue

Section

Regular Articles

License

Authors who publish with this journal agree to the following terms:

  • Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution License that allows others to share the work with an acknowledgement of the work's authorship and initial publication in this journal.
  • Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgement of its initial publication in this journal.
 

Most read articles by the same author(s)