Premium
Structure‐Activity Relationships in a Series of 8‐Substituted Xanthines as Bronchodilator and A 1 ‐Adenosine Receptor Antagonists
Author(s) -
Corsano Stefano,
Strappaghetti Giovannella,
Scapicchi Rossana,
Lucacchini Antonio,
Senatore Generoso
Publication year - 1995
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19953280905
Subject(s) - theophylline , xanthine , chemistry , bronchodilator , piperazine , adenosine , adenosine receptor , adenosine a1 receptor , stereochemistry , agonist , pharmacology , receptor , biochemistry , medicine , enzyme , organic chemistry , biology , asthma
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.