化学
甲状腺激素受体
体内
化学合成
立体化学
激素
受体
兴奋剂
选择性
药理学
体外
生物化学
医学
生物
生物技术
催化作用
作者
Timothy P. Burkholder,Brian E. Cunningham,Joshua R. Clayton,Peter A. Lander,Matthew L. Brown,Robert A. Doti,Gregory L. Durst,Chahrzad Montrose‐Rafizadeh,Constance King,Harold E. Osborne,Robert M. Amos,Richard W. Zink,Lawrence E. Stramm,Thomas P. Burris,Guemalli R. Cardona,Debra L. Konkol,Charles A. Reidy,Michael E. Christe,Michaël Génin
标识
DOI:10.1016/j.bmcl.2015.02.062
摘要
The design, synthesis, and structure activity relationships for a novel series of indoles as potent, selective, thyroid hormone receptor β (TRβ) agonists is described. Compounds with >50× binding selectivity for TRβ over TRα were generated and evaluation of compound 1c from this series in a model of dyslipidemia demonstrated positive effects on plasma lipid endpoints in vivo.
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