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


Akgün H., Balkan A., EROL K., Batu Ö. S.

Arzneimittel-Forschung/Drug Research, vol.48, no.6, pp.658-662, 1998 (SCI-Expanded, Scopus)

  • Publication Type: Article / Article
  • Volume: 48 Issue: 6
  • Publication Date: 1998
  • Journal Name: Arzneimittel-Forschung/Drug Research
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.658-662
  • Keywords: 2,4- Pentanediones, 3,5-Dimethylisoxazoles, Antiasthmatic drugs, Antihistaminic drugs, Theophylline, bronchodilator activity, Xanthine derivatives
  • Kütahya Health Sciences University Affiliated: Yes

Abstract

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.