芳香族二羟基化螺[茚满-1,3'-吡咯烷]和螺[茚满-2,2'-吡咯烷]衍生物的合成与药理评价
Synthesis and pharmacological evaluation of aromatic dihydroxylated spiro[indan-1,3'-pyrrolidine] and spiro[indan-2,2'-pyrrolidine] derivatives.
作者信息
Sommerville R, Rosenberg H E, Crooks P A
出版信息
J Pharm Sci. 1985 May;74(5):553-5. doi: 10.1002/jps.2600740512.
PMID:4020632
Abstract
Aromatic hydroxylated derivatives of the spiro[indan-1,3'-pyrrolidine] and spiro[indan-2,2'-pyrrolidine] ring systems have been synthesized and evaluated for dopaminergic agonist and antagonist activities. None of these conformationally restricted catecholamines possessed any dopaminergic activity, but 5,6-dihydroxy spiro[indan-1,3'-pyrrolidine] hydrobromide exhibited weak dopamine antagonist properties.
摘要
已合成了螺[茚满-1,3'-吡咯烷]和螺[茚满-2,2'-吡咯烷]环系的芳香羟基化衍生物，并对其多巴胺能激动剂和拮抗剂活性进行了评估。这些构象受限的儿茶酚胺均不具有任何多巴胺能活性，但5,6-二羟基螺[茚满-1,3'-吡咯烷]氢溴酸盐表现出较弱的多巴胺拮抗剂特性。
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Synthesis and pharmacological evaluation of aromatic dihydroxylated spiro[indan-1,3'-pyrrolidine] and spiro[indan-2,2'-pyrrolidine] derivatives.芳香族二羟基化螺[茚满-1,3'-吡咯烷]和螺[茚满-2,2'-吡咯烷]衍生物的合成与药理评价
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