A series of 4-(3,4-dihydroxyphenyl)-1,2,3,4-tetrahydroisoquinoline derivatives showed potent DA1 agonistic activities. We investigated the structure-activityrelationship of the racemic compounds of this series. 4-(3,4-Dihydroxyphenyl)-7-methanesulfonamido-1,2,3,4-tetrahydroiso quinoline (43) was identified as a potent renal vasodilator with activity almost equal to that of YM435 (1).
SUBSTITUTED ISOQUINOLINES AND THEIR USE AS TUBULIN POLYMERIZATION INHIBITORS
申请人:Leblond Bertrand
公开号:US20130131018A1
公开(公告)日:2013-05-23
The present invention relates generally to substituted isoquinolines and their use as tubulin polymerization inhibitors. In particular, the invention relates to substituted isoquinolines which possess useful therapeutic activity, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds.