132560-04-4Relevant articles and documents
Structure-activity relationships in a series of xanthine derivatives with antibronchoconstrictory and bronchodilatory activities
Merlos,Gomez,Vericat,Bartroli,Garcia-Rafanell,Forn
, p. 653 - 658 (2007/10/02)
Thirty-one 1,3,7,8-substituted xanthine derivatives have been synthesized and evaluated for bronchodilator and anti-bronchoconstrictory activities in in vitro tracheal relaxation and in vivo bronchospasm inhibition models. Activity tests have been complemented with phosphodiesterase inhibition and toxicological data. Structure-activity relationships are discussed. Compound 21 (1,3-diisobutyl-8-methylxanthine) has been selected for further pharmacological development because of its good activity profile and favourable therapeutic index, which is 14- and 38-fold greater than that of theophylline and IBMX, respectively.