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Updated: Aug 21, 2026

Preparation of Enantiopure Non-Activated Aziridines and Synthesis of Biemamide B, D, and epiallo-Isomuscarine
Published on: June 13, 2022
Synthesis and biological evaluation of some 6-arylamidomorphines as analogues of morphine-6-glucuronide
James M Macdougall1, Xiao-Dong Zhang, Willma E Polgar
1Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121-2804, USA. jmacdougall@hbri.org
Abstract:
A series of 6-beta-arylamidomorphines was synthesized and biologically evaluated. Various aryl substituents were introduced into the arylamidomorphines to examine substituent structure-activity relationships. Competition binding assays showed that compounds 10a-h bound to the mu opioid receptor with high affinity (0.2-0.6 nM). Functional assays showed that compounds 10a-h acted as full mu opioid receptor agonists. The ED(50) of compound 10e.HCl as an analgesic was 12.6 mg/kg in the tail flick latency test in the rat.
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