Bioorganic & medicinal chemistry

Substituted 1, 2, 3, 4-tetrahydroquinolin-6-yloxypropanes as β 3-adrenergic receptor agonists: Design, synthesis, biological evaluation and pharmacophore modeling

N Shakya, KK Roy, AK Saxena

文献索引：Shakya, Neeraj; Roy, Kuldeep K.; Saxena, Anil K. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 2 p. 830 - 847

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被引用次数: 21

摘要

In search of potent β3-adrenergic receptor agonists, a series of novel substituted 1, 2, 3, 4- tetrahydroquinolin-6-yloxypropanes has been synthesized and evaluated for their β3- adrenergic receptor agonistic activity (ranging from− 17.73% to 90.64% inhibition at 10μM) using well established Human SK-N-MC neuroblastoma cells model. Four molecules viz. 11, 15, 22 and 23 showed β3-AR agonistic IC50 value of 0.55, 0.59, 1.18 and 1.76 μM, ...