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STRUCTURE‐ACTIVITY RELATIONSHIPS IN A SERIES OF 6‐THIOXANTHINES WITH BRONCHODILATOR AND CORONARY DILATOR PROPERTIES
Author(s) -
ARMITAGE A. K.,
BOSWOOD JANET,
LARGE B. J.
Publication year - 1961
Publication title -
british journal of pharmacology and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0366-0826
DOI - 10.1111/j.1476-5381.1961.tb01279.x
Subject(s) - dilator , bronchodilator , bronchodilator agents , medicine , bronchodilation , pharmacology , stimulant , cardiology , anesthesia , asthma
The bronchodilator activity of 47 compounds on the isolated guinea‐pig tracheal ring preparation and the coronary dilator activity on the dog heart‐lung preparation is described. 1,3‐Disubstituted xanthines and 6‐thioxanthines (theophyllines and 6‐thiotheophyllines) were more active as bronchodilators and as coronary dilators than were 3,7‐disubstituted 6‐thioxanthines (6‐thiotheobromines) or 1,3,7‐trisubstituted 6‐thioxanthines (6‐thiocaffeines). None of the 6‐thioxanthines was of any interest as a diuretic and none of the 6‐thiocaffeines was of any interest as a central stimulant. Structure‐activity requirements for potent bronchodilator and coronary dilator activity are discussed.