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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Conformationally restrained analogues of sympathomimetic catecholamines. Synthesis and adrenergic activity of 5,6- and 6,7-dihydroxy-3,4-dihydrospiro(naphthalen-1(2H)-2',5'-morpholines).
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Conformationally restrained analogues of sympathomimetic catecholamines. Synthesis and adrenergic activity of 5,6- and 6,7-dihydroxy-3,4-dihydrospiro(naphthalen-1(2H)-2',5'-morpholines).

机译：拟交感神经儿茶酚胺的构象受限类似物。 5,6-和6,7-二羟基-3,4-二氢螺（萘-1（2H）-2'，5'-吗啉）的合成和肾上腺素活性。

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摘要

The 5,6- (10a) and 6,7-dihydroxy-3,4-dihydrospiro[naphthalen-1(2H)-)-2',5'-morpholine](11a) and their N-isopropyl derivatives (10b and 11b) (DDSNMs), which can be viewed as the result of the combination of the structure of the 2-(3,4-dihydroxyphenyl)morpholine 5a or 5b (DPMs) with the structure of the corresponding 1-(aminomethyl)-5,6-dihydroxy- (8a or 8b) or 1-(aminomethyl)-6,7-dihydroxy-1,2,3,4-tetrahydro-1-naphthalen-ol (9a or 9b) (1-AMDTNs) were synthesised. The new compounds DDSNMs 10a,b and 11a,b were assayed for their alpha- and beta-adrenergic properties by means of binding experiments and functional tests and the results were compared with those obtained for catecholamines 1a, b and the previously described morpholine (5) and tetrahydronaphthalene (8, 9) derivatives. The affinity and activity indices thus obtained indicate in general a low ability of the new compounds 10 and 11 to interact with the alpha- and beta-adrenoceptors, which, in all cases, was lower than that of the corresponding morpholine (5) and tetrahydronaphthalene (8, 9) analogues.
机译：5,6-（10a）和6,7-二羟基-3,4-二氢螺[萘-1（2H）-）-2'，5'-吗啉]（11a）及其N-异丙基衍生物（10b和11b）（DDSNMs），可以看作是2-（3,4-二羟基苯基）吗啉5a或5b（DPMs）结构与相应的1-（氨基甲基）-5结构结合的结果合成了6-6-二羟基-（8a或8b）或1-（氨基甲基）-6,7-二羟基-1,2,3,4-四氢-1-萘酚（9a或9b）（1-AMDTNs） 。通过结合实验和功能测试分析了新化合物DDSNMs 10a，b和11a，b的α-和β-肾上腺素能，并将结果与​​儿茶酚胺1a，b和先前所述的吗啉进行了比较（5 ）和四氢萘（8，9）衍生物。由此获得的亲和力和活性指数通常表明新化合物10和11与α-和β-肾上腺素受体相互作用的能力低，在所有情况下，其均低于相应的吗啉（5）和四氢萘的能力。 （8，9）类似物。

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