79730-42-0Relevant academic research and scientific papers
New Antihistaminic Theophylline or Theobromine Derivatives
Pascal, Jean-Claude,Beranger, Serge,Pinhas, Henri,Poizot, Alain,Desiles, Jean-Pierre
, p. 647 - 652 (2007/10/02)
A series of 3,4-dihydro-1,3-dimethyl-7--1H-purine-2,6-diones and 3,7-dihydro-3,7-dimethyl-1--1H-purine-2,6-diones was synthesized and evaluated for antihistaminic activity.Some of them displayed good inhibition of both histamine-induced bronchospasm in the anesthetized guinea pig at 10 μ/kg by the intravenous route and of passive cutaneous anaphylaxis in the rat at 10 mg/kg by the oral route.Comparison of the two most active compounds revealed a higher antihistaminic activity with the compounds containing a (phenylthio)propyl group (1 and 2) as compared with that containing a phenoxy group.Compound 2 piperazin-1-yl>-2-hydroxypropyl>-1H-purine-2,6-dione> was selected for clinical trials on the basis of a comparative pharmacological study with chloropheniramine, ketotifen, promethazine, and theophylline.
