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首页> 外文期刊>Journal of Medicinal Chemistry >Effect of the 3- and 4?Methyl Groups on the Opioid Receptor Properties of N?Substituted trans-3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines
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Effect of the 3- and 4?Methyl Groups on the Opioid Receptor Properties of N?Substituted trans-3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines

机译：3-和4-甲基对N 3取代的反式3，4-二甲基-4-（3-羟苯基）哌啶类阿片受体性质的影响

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摘要

N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines (2a,b) are opioid receptor antagonists where the antagonist properties are not due to the type of N-substituent. In order to gain a better understanding of the contribution that the 3- and 4-methyl groups make to the pure antagonist properties of 2a,b, we synthesized analogues of 2a,b that lacked the 4-methyl (5a,b), 3-methyl (6a,b), and both the 3- and 4-methyl group (7a,b) and compared their opioid receptor properties. We found that (1) all N-methyl and N-phenylpropyl substituted compounds were nonselective opioid antagonists (2) all N-phenylpropyl analogues were more potent than their N-methyl counterparts, and (3) compounds 2a,b which have both a 3- and 4-methyl substituent, were more potent antagonists than analogues 5a,b, 6a,b, and 7a,b. We also found that the removal of 3-methyl substituent of N-methyl and N-phenylpropyl 3-methyl-4-(3-hydroxyphenyl)piperazines (8a,b) gives (4a,b), which are opioid antagonists.
机译：N-取代的反式-3,4-二甲基-4-（3-羟苯基）哌啶（2a，b）是阿片类受体拮抗剂，其拮抗剂特性并非由于N-取代基的类型而引起。为了更好地理解3-和4-甲基对2a，b的纯拮抗剂特性的贡献，我们合成了缺少4-甲基（5a，b），3的2a，b类似物。 -甲基（6a，b），以及3-和4-甲基（7a，b），并比较了它们的阿片受体特性。我们发现（1）所有N-甲基和N-苯基丙基取代的化合物均为非选择性阿片类拮抗剂（2）所有N-苯基丙基类似物均比其N-甲基类似物更有效，（3）化合物2a，b同时具有a 3-和4-甲基取代基比类似物5a，b，6a，b和7a，b更有效。我们还发现，除去N-甲基和N-苯基丙基3-甲基-4-（3-羟基苯基）哌嗪（8a，b）的3-甲基取代基可得到（4a，b），这是阿片类拮抗剂。

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