Synthesis and pharmacological evaluation of 6,7-indolo/thiazolo-morphinans--further SAR of levorphanol.
Synthesis and pharmacological evaluation of 6,7-indolo/thiazolo-morphinans--further SAR of levorphanol.
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6,7-吲哚/噻唑吗啡喃的合成和药理评价——左啡诺的进一步SAR。
DOI:
10.1021/jm0701674
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发表时间:
2007
影响因子:
7.3
通讯作者:
Neumeyer,JohnL
中科院分区:
文献类型:
--
作者:
Zhang,Ao;Li,Fuying;Ding,Chunyong;Yao,Qizhen;Knapp,BrianI;Bidlack,JeanM;Neumeyer,JohnL
To further extend the structure−activity relationships of levorphanol, two series of novel morphinans were prepared by incorporation of an indole or aminothiazole fragment to the hexyl ring (ring C) in levorphanol. Such morphinans differed from previously reported ligands in that such indole- or aminothiazole-containing morphinans displayed enhanced binding affinity to the δ opioid receptor, while the affinity to κ and μ receptors was slightly reduced.