New beta-diketone and 3,5-dimethyl isoxazole derivatives of theophylline as potential bronchodilator agents.
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.
Hacettepe University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ankara, Turkey.
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H
Akgün
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Balkan
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Erol
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Batu
D000109:Acetylcholine / Q000037:antagonists & inhibitors / Q000494:pharmacology; D000818:Animals; D001980:Bronchi / Q000187:drug effects; D001993:Bronchodilator Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D005260:Female; D006168:Guinea Pigs; D006632:Histamine / Q000494:pharmacology; D006633:Histamine Antagonists / Q000494:pharmacology; D066298:In Vitro Techniques; D007555:Isoxazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D013806:Theophylline / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*
D001993:Bronchodilator Agents; D006633:Histamine Antagonists; D007555:Isoxazoles; D006632:Histamine; D013806:Theophylline; D000109:Acetylcholine