New beta-diketone and 3,5-dimethyl isoxazole derivatives of theophylline as potential bronchodilator agents

Akgun H., Balkan A., Erol K., Batu O.

ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH, vol.48, no.6, pp.658-662, 1998 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 48 Issue: 6
  • Publication Date: 1998
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Index Chemicus (IC)
  • Page Numbers: pp.658-662
  • Keywords: antiasthmatic drugs, antihistaminic drugs, 3,5-dimethylisoxazoles, 2,4-penta-nediones, theophylline, bronchodilator activity, xanthine derivatives
  • Anadolu University Affiliated: No


Ten new compounds having 7-[(2,4-pentanedione-3-yl)alkyl]- and 7-[(3,5-dimethylisoxazole-4-yl)alkyl]-3,7-dihydro-1,3-dimethyl-1H-purine-2,6-dione structures were synthesized and their bronchodilator activities investigated using the method based on inhibition of acetylcholine and histamine-induced contractions in guinea pig trachea. None of the compounds were effective on acetylcholine-induced contractions. However, the compounds 4d, 4e, 5d and 5c were potent inhibitors of the bronchospasm induced by histamine, whereas the others (4b, 4c, 5b and 5c) were weak inhibitors.