Design and synthesis of 10-oxo derivative of N-cyclopropylmethyl (−)-6β-acetylthiodihydro-normorphine, a potentially κ-selective opioid receptor ligand

The design and synthesis of 10-oxo derivative of N-cyclopropylmethyl-(−)-6β-acetylthio dihydronormorphine ( 4) are described. The result of pharmacological assays indicate that compound 4 acts as a μ-opioid receptor antagonist and κ-opioid receptor agonist which is suggested to be more potent analge...

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Published inBioorganic & medicinal chemistry letters Vol. 5; no. 14; pp. 1505 - 1508
Main Authors Sagara, Takeshi, Ozawa, Sawako, Kushiyama, Emi, Koike, Katsuo, Takayanagi, Issei, Kanematsu, Ken
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 20.07.1995
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Summary:The design and synthesis of 10-oxo derivative of N-cyclopropylmethyl-(−)-6β-acetylthio dihydronormorphine ( 4) are described. The result of pharmacological assays indicate that compound 4 acts as a μ-opioid receptor antagonist and κ-opioid receptor agonist which is suggested to be more potent analgesic action than that of 1 and morphine through an activation of κ-opioid receptors. The design and synthesis of 10-oxo derivative of N-cyclopropylmethyl-(−)-6β-acetylthio dihydronormorphine ( 4) and its biological assays are described.
ISSN:0960-894X
1464-3405
DOI:10.1016/0960-894X(95)00239-P