Design, Synthesis, and Biological Evaluation of 14-Heteroaromatic-Substituted Naltrexone Derivatives: Pharmacological Profile Switch from Mu Opioid Receptor …

…, SA Zaidi, O Elbegdorj, LCK Aschenbach…

文献索引：Yuan, Yunyun; Zaidi, Saheem A.; Elbegdorj, Orgil; Aschenbach, Lindsey C. K.; Li, Guo; Stevens, David L.; Scoggins, Krista L.; Dewey, William L.; Selley, Dana E.; Zhang, Yan Journal of Medicinal Chemistry, 2013 , vol. 56, # 22 p. 9156 - 9169

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被引用次数: 8

摘要

On the basis of a mu opioid receptor (MOR) homology model and the isosterism concept, three generations of 14-heteroaromatically substituted naltrexone derivatives were designed, synthesized, and evaluated as potential MOR-selective ligands. The first- generation ligands appeared to be MOR-selective, whereas the second and the third generation ones showed MOR/kappa opioid receptor (KOR) dual selectivity. Docking of ...