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一些被设计为普罗法多刚性类似物的螺[茚满-1,3'-吡咯烷]衍生物的合成与镇痛活性

The synthesis and analgesic activities of some spiro[indan-1,3'-pyrrolidine] derivatives designed as rigid analogs of profadol.

作者信息

Crooks P A, Sommerville R

出版信息

J Pharm Sci. 1982 Mar;71(3):291-4. doi: 10.1002/jps.2600710306.

DOI:10.1002/jps.2600710306
PMID:6461753
Abstract

Aromatic hydroxylated derivatives of spiro[indan-1,3'-pyrrolidine], designed as conformationally restricted analogs of profadol, were synthesized and pharmacologically evaluated in mice for analgesia and other central nervous system activities. None of the compounds synthesized were as potent as profadol in writhing and hot plate tests, but the 4-hydroxy derivative exhibited codeine-level analgesia in the tests.

摘要

螺[茚满-1,3'-吡咯烷]的芳香族羟基化衍生物被设计为普罗法多的构象受限类似物，已合成并在小鼠身上进行了镇痛及其他中枢神经系统活性的药理学评估。在扭体和热板试验中，所合成的化合物均不如普罗法多有效，但4-羟基衍生物在试验中表现出与可待因相当的镇痛效果。

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1
The synthesis and analgesic activities of some spiro[indan-1,3'-pyrrolidine] derivatives designed as rigid analogs of profadol.一些被设计为普罗法多刚性类似物的螺[茚满-1,3'-吡咯烷]衍生物的合成与镇痛活性
J Pharm Sci. 1982 Mar;71(3):291-4. doi: 10.1002/jps.2600710306.
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Synthesis and analgesic properties of some conformationally restricted analogues of profadol.普罗法朵某些构象受限类似物的合成及镇痛特性
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Synthesis of spiro[tetralin-2,2'-pyrrolidine] and spiro[indan-2,2'-pyrrolidine] derivatives as potential analgesics.螺[四氢萘-2,2'-吡咯烷]和螺[茚满-2,2'-吡咯烷]衍生物作为潜在镇痛药的合成。
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