Basic Information
ID: ALA1134426
Journal: Bioorg Med Chem Lett
Title: Derivatives of 17-(2-methylallyl)-substituted noroxymorphone: variation of the delta address and its effects on affinity and selectivity for the delta opioid receptor.
Authors: Ullrich T, Dersch CM, Rothman RB, Jacobson AE, Rice KC.
Abstract: In an effort to establish the importance of the N-(2-methylallyl) substituent in the noroxymorphone series, several derivatives have been synthesized, retaining that N-substituent and modifying the delta address moiety. A few compounds showed moderate binding affinity and selectivity for the delta receptor; none displayed a pharmacological profile as exceptional as N-(2-methylallyl)noroxymorphindole. A second study showed that 3-O-methylation of all derivatives decreases binding affinity. The present results indicate that only a combination of the N-(2-methylallyl) group and an indole delta address provided high selectivity for the delta receptor.
CiteXplore: 11597422
DOI: 10.1016/s0960-894x(01)00580-7
Patent ID: ┄
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