新型杂环甲状腺激素模拟物。第2部分。
Novel heterocyclic thyromimetics. Part 2.
作者信息
Haning Helmut, Mueller Ulrich, Schmidt Gunter, Schmeck Carsten, Voehringer Verena, Kretschmer Axel, Bischoff Hilmar
机构信息
Bayer HealthCare AG, Bayer Schering Pharma Global Drug Discovery, D-42096 Wuppertal, Germany.
出版信息
Bioorg Med Chem Lett. 2007 Jul 15;17(14):3992-6. doi: 10.1016/j.bmcl.2007.04.085. Epub 2007 Apr 29.
Novel heterocyclic thyromimetics are presented carrying carboxy-substituted benzofurans or sulfur containing heterocycles, as replacements for the amino acid side chain of T3. Potent agonists were identified in both series. SAR trends are examined and found to be mostly consistent with previously published thyromimetics. The lack of isoform selectivity demonstrated with isoform-selective transient THR transfection assays has been confirmed by corresponding in vivo studies.
新型杂环甲状腺激素模拟物被呈现出来，其带有羧基取代的苯并呋喃或含硫杂环，作为T3氨基酸侧链的替代物。在这两个系列中都鉴定出了强效激动剂。研究了构效关系趋势，发现其大多与先前发表的甲状腺激素模拟物一致。通过相应的体内研究证实了在亚型选择性瞬时THR转染试验中所表现出的缺乏亚型选择性。
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