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Medetomidine analogs as α2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of medetomidine analogs and their potential binding …

…, JE De Los Angeles, MY He, JT Dalton…

文献索引:Zhang, Xiaoyan; De Los Angeles, Joseph E.; He, Mei-Ying; Dalton, James T.; Shams, Gamal; Lei, Longping; Patil, Popat N.; Feller, Dennis R.; Miller, Duane D.; Hsu, Fu-Lian Journal of Medicinal Chemistry, 1997 , vol. 40, # 19 p. 3014 - 3024

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被引用次数: 23

摘要

The synthesis and the biological evaluation of a new series of medetomidine analogs are reported. The substitution pattern at the phenyl ring of the tetralin analogs had a distinct influence on the α2-adrenoceptor binding affinity. 4-Methylindan analog 6 was the most potent α2-adrenoceptor binding ligand among these 4-substituted imidazoles, and its α2- adrenoceptor selectivity was greater than the 5-methyl tetralin analog 4c. Ligand- ...