Four new derivatives of 8-piperazine ethyl xanthine were synthesized and their bronchospasmolytic activity and A(1)-adenosine affinity were studied. Their relaxant action in the tracheal muscle was lower than that of theophylline and that of theophylline derivatives substituted at the 7-position. Only compound 9, where the methyl group in the 1-position of the theophylline was substituted by an isobutyl group, shows a good affinity towards the A(1)-adenosine receptor.
Structure-activity relationships in a series of 8-substituted xanthines as bronchodilator and A(1)-adenosine receptor antagonists
LUCACCHINI, ANTONIO;
1995-01-01
Abstract
Four new derivatives of 8-piperazine ethyl xanthine were synthesized and their bronchospasmolytic activity and A(1)-adenosine affinity were studied. Their relaxant action in the tracheal muscle was lower than that of theophylline and that of theophylline derivatives substituted at the 7-position. Only compound 9, where the methyl group in the 1-position of the theophylline was substituted by an isobutyl group, shows a good affinity towards the A(1)-adenosine receptor.File in questo prodotto:
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