Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine
摘要:
A synthesis of all four diastereoisomeric 3-(tert-butoxycarbonyl)-1,6-dimethoxyoctahydrobenzo[g]quinolines 13a-d is presented. The two trans isomers 13b and 13c have been converted to tricyclic analogues 20 (CV 205-502) and 26 (205-503) of the potent dopaminomimetic ergolines CQ 32-084 and pergolide, respectively. These two compounds combine the essential moiety of apomorphine with the important 8-substituents of ergolines. Preliminary pharmacological evaluation of 20 and 26 suggests that these novel dopamine agonists combine the specificity of apomorphine with the potency, long duration of action, and good oral activity of the ergolines.
Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine
摘要:
A synthesis of all four diastereoisomeric 3-(tert-butoxycarbonyl)-1,6-dimethoxyoctahydrobenzo[g]quinolines 13a-d is presented. The two trans isomers 13b and 13c have been converted to tricyclic analogues 20 (CV 205-502) and 26 (205-503) of the potent dopaminomimetic ergolines CQ 32-084 and pergolide, respectively. These two compounds combine the essential moiety of apomorphine with the important 8-substituents of ergolines. Preliminary pharmacological evaluation of 20 and 26 suggests that these novel dopamine agonists combine the specificity of apomorphine with the potency, long duration of action, and good oral activity of the ergolines.
Novel pharmaceutically active 1,2,3,4,4a,5,10,10a-octahydrobenzo(g)quinoline derivatives
申请人:SANDOZ AG
公开号:EP0077754A2
公开(公告)日:1983-04-27
A 6- and/or 7-oxy-trans-1,2,3,4,4a,5,10,10a-octahydro- benzo[g]-quinoline in which the 3-position is substituted by an optionally amidated carboxy group, an optionally etherified hydroxymethyl group, a cyanomethyl group, an alkyl-or aryl-thiomethyl group or a sulfamoylamino or carbamoylamino group, or a physiologically-hydrolysable and -acceptable ester thereof. The subject compounds are useful as pharmaceuticals, in particular as prolactin secretion inhibitors, dopaminergic agents and dopamine receptor stimulating agents.
Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine
作者:Rene Nordmann、Trevor J. Petcher
DOI:10.1021/jm00381a017
日期:1985.3
A synthesis of all four diastereoisomeric 3-(tert-butoxycarbonyl)-1,6-dimethoxyoctahydrobenzo[g]quinolines 13a-d is presented. The two trans isomers 13b and 13c have been converted to tricyclic analogues 20 (CV 205-502) and 26 (205-503) of the potent dopaminomimetic ergolines CQ 32-084 and pergolide, respectively. These two compounds combine the essential moiety of apomorphine with the important 8-substituents of ergolines. Preliminary pharmacological evaluation of 20 and 26 suggests that these novel dopamine agonists combine the specificity of apomorphine with the potency, long duration of action, and good oral activity of the ergolines.