Synthesis of new salicylamide derivatives with evaluation of their antiinflammatory, analgesic and antipyretic activities

  • H. H. Fahmy
  • G. A. Soliman
Research Article Medicinal Chemistry & Natural Products


A new series of pyridazine, pyrazoles, pyrazolidine-3,5-dione, Semicarbazide, thiosemicarbazides, hydantoin, thiohydantoins, 1,2,4-triazoles, S-triazolo[3,4-b]-1,3,4-thiadiazoles incorporated indirectly into salicylamide moiety at position 2 were synthesized. Also the synthesis of novel series of 3-salicylamido-2-hydroxypropyl-amine derivatives were prepared. Several of these compounds were screened for antiinflammatory, analgesic, antipyretic and ulcerogenic activities.

Key words

Salicylamide derivatives 1,2,4-Triazoles S-Triazolo[3,4-b]-1,3,4-thiadiazoles pyrazoles Antiinflammatory analgesic and antipyretic activities 


  1. Abdel Motti, F. M., Abdel Megeid, M. E., Zaki, M. E., and Shamrokh, A. H., Synthesis of 3-heterocyclic 5,6-diphenylpyridazines.Egypt. J. Pharm. Sci., 38(1–3), 87–93 (1997).Google Scholar
  2. Amin, K. M., El-Shafie F. S., and El-Tahir, K. E. H., Synthesis and antiallergic activity of some coumarinyloxy-amines. ibid, 34(4–6) 787–804 (1993).Google Scholar
  3. Coleman, D. L., Wood, N. L., and Darling, W. M., Martindale the Extrapharmacopoei Edited by James E. E. Reynolds Published by Direction of the Council of Royal Pharmaceutical Society of Great Britain, Thirtieth Edition, 1–36 (1993).Google Scholar
  4. Corell, T., Moller, J. K., and Splawinski, J., A New Antiinflammatory Derivative of Indiazole which is less ulcerogenic than indomethacin in Rats,Acta pharmacol, er. Toxicol, 45, 232–239 (1979).Google Scholar
  5. Daidone, G., Raffa, D., and Plescia, S., Synthesis and evaluation of analgesic and antiinflammatory activities ofN-substituted salicylamides.IL Farmaco 44(5) 465–473 (1989).PubMedGoogle Scholar
  6. El-Ansary, S. L. and Hassan, A. B., Synthesis and biological activity of some new thiadiazolo, triazolo and fused S-triazolo[3,4-b]-1,3,4-thiadiazolo coumarins.Egypt J. Pharm. Sci., 35(1–6), 267–287 (1994).Google Scholar
  7. El-Hakim A. E. and Ain-Shoka A. A., Synthesis and pharmacological activity of certain “N-Arylanthranilic acid esters”. ibid, 36(1–6), 55–70 (1995).Google Scholar
  8. Fahmy, H. H., Synthesis of some new quinoline derivatives of potential antimicrobial activity. ibid, 38(4–6), 403–414 (1997).Google Scholar
  9. Fahmy, H. H., W. Abdou, A. M., and El-Eraky, W., Synthesis of some new pyrazolones as potent antiinflammatory agent.Bull Fac. Pharm Cairo univ. 33 (3) 85–91 (1995).Google Scholar
  10. Fahmy, H. H. and El-Eraky, W., Synthesis and evaluation of the analgesic and antiinflammatory activities ofO-substituted Salicylamides.Arch. Pharm. Res., 24, 171–179 (2001).PubMedGoogle Scholar
  11. Joullie, Maurice, Maillord, Gabriel (Recherches pharmaceutiques et Scientifiques and Omnium chimique S. A.). Ger. offen. 2,106, 509. β-adrenergic blocking (aryloxy) propanolamines.Chem. Abst. 75, 140515V (1971).Google Scholar
  12. Modi, K. F., Krishnakumar, H. J., Mehta, A. C., Padhya, and Somasekhara, S., “Synthesis of S-(4-Aryl-4H-1,2-4-triazol-3-yl)-2-mercaptomethylbenz-imidazoles.”J. Indian Chem. Soc., 54(7), 741–742 (1977).Google Scholar
  13. Mody, M. K., Prasad, A. R., Ramalingam, T. and Sattur, P. B. “Synthesis and pharmacology of 2-aryl-5-aryloxy-alkyl-S-triazolo[3,4-b]-1,3,4-thiadiazoles”. ibid, 59, 769–770 (1982).Google Scholar
  14. Mueckter, Heinrich (Chemie Gruenenthal G. m. b. H.) Ger offen. Pharmaceutical composition containing 1, 2,4- triazole-3-carboxylic acid amides, for treatment of arthritis and rheumatism. 2,533,926 (cl, A61 k31/41) 17 Feb. 1977,Chem. Abst. 86. 133786 h (1977).Google Scholar
  15. Omar, M. T., Synthesis of new xanthenone derivatives of expected antibilharzial activity.Arch. Pharm. Res., 20 (6), 602–609, (1997).CrossRefPubMedGoogle Scholar
  16. Pant, M. K., Durgapal R., and Joshi, P. C., Synthesis and Fungicidal activity of some new indole derivatives.Indian J. Chem., 22b, 712–713 (1983).Google Scholar
  17. Snedecol, W. G., and Cochran, G. W., Statistical method, Iowa state university, press, Ames., Lowa state Ames., (1971).Google Scholar
  18. Tominage, Y., Honkawa, Y., Hare, M. and Hosomi, A., Synthesis of pyrazolo[3,4-d]pyrimidine derivatives using ketene dithioacetals.J. Heterocyclic Chem., 27, 775 (1990).Google Scholar
  19. Van Reet, Gustaaf., Heeres, Jan, Wals, Lourens (Janssen pharmaceutica N. V); Antimicrobial and plant-growth regulating triazole derivatives. U. S. Patent 4, 160, 838 (Cl., 424–269; A01 Ng/22) 10 Jul 1979,Chem. Abst., 91, 175361z (1979).Google Scholar
  20. Wade, P. C., Vogt, B. R., and Kissick, T. P., (Squibb, E. R., and Sons Inc.) Antiinflammatory 1-acyl-3(5)-alkyl-5(3)-phenyl-1,2–4-triazoles. U.S. Patent 4, 154, 841 (cl. 424, 269; A61 k31/41) 15 May 1979.,Chem. Abst., 91, 74655t (1979).Google Scholar
  21. Winter, C. A., Risleye, A. A., and Nuss, G. W., Carrageenan induced oedema in Hind Paw of the Rat as an Assay for Antiinflammatory Drug.Proc. Soc. Exp. Biol. Med., 111, 544–547 (1962).PubMedGoogle Scholar

Copyright information

© The Pharmaceutical Society of Korea 2001

Authors and Affiliations

  1. 1.Therapeutical Chemistry DepartmentNational Research CentreDokki, CairoEgypt
  2. 2.Faculty Vet. Med., Dept. of PharmacologyCairo UniversityEgypt

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