STRUCTURE-ACTIVITY-RELATIONSHIPS IN A SERIES OF XANTHINE DERIVATIVES WITH ANTIBRONCHOCONSTRICTORY AND BRONCHODILATORY ACTIVITIES

被引：18

作者：

MERLOS, M

GOMEZ, L

VERICAT, ML

BARTROLI, J

GARCIARAFANELL, J

FORN, J

机构：

[1] J URIACH & CIA SA,DEPT PHARMACOL,DEGA BAHI 59-67,E-08026 BARCELONA,SPAIN

[2] J URIACH & CIA SA,RES CTR,DEPT CHEM,E-08026 BARCELONA,SPAIN

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1990年 / 25卷 / 08期

关键词：

antibronchoconstrictory activity; bronchodilatory; phosphodiesterase inhibition; xanthine derivatives;

D O I：

10.1016/0223-5234(90)90130-U

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Thirty-one 1,3,7,8-substituted xanthine derivatives have been synthesized and evaluated for bronchodilator and antibronchoconstrictory 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. © 1990.

引用

页码：653 / 658

页数：6

共 19 条

[1] RELATIONSHIPS BETWEEN ADENOSINE, CYCLIC-NUCLEOTIDES, AND XANTHINES IN ASTHMA [J].