Zhang Ao, Li Fuying, Ding Chunyong, Yao Qizhen, Knapp Brian I, Bidlack Jean M, Neumeyer John L
Bioorganic and Medicinal Chemistry Laboratory, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
J Med Chem. 2007 May 31;50(11):2747-51. doi: 10.1021/jm0701674. Epub 2007 May 9.
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 delta opioid receptor, while the affinity to kappa and micro receptors was slightly reduced.
为了进一步拓展左啡诺的构效关系，通过将吲哚或氨基噻唑片段引入左啡诺的己基环（C环），制备了两个系列的新型吗啡喃。这类吗啡喃与先前报道的配体不同，在于这类含吲哚或氨基噻唑的吗啡喃对δ阿片受体表现出增强的结合亲和力，而对κ和μ受体的亲和力略有降低。
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