N-甲基硫脲作为维甲酸受体相关孤儿受体的新型激动剂。
N-methylthioureas as new agonists of retinoic acid receptor-related orphan receptor.
机构信息
College of Pharmacy, Inje University, 607 Obang-dong, Gimhae, Gyeongnam, 621-749, Korea.
出版信息
Arch Pharm Res. 2012 Aug;35(8):1393-401. doi: 10.1007/s12272-012-0809-0. Epub 2012 Sep 1.
Thirty two thiourea derivatives were prepared and their agonistic activities on the retinoic acid receptor-related orphan receptor α (RORα) were evaluated. The replacement of the 3-allyl-2-imino-thiazolidin-4-one moiety of the lead compound CGP52608 (1) with various functional group substituted aromatic rings, improved the agonistic activity of RORα. Among the prepared derivatives, 1-methyl-3-(4-phenoxy-benzyl)-thiourea (32) showed 2.6-fold higher agonistic activity than CGP52608 in the RORα-activation assay.
三十二种硫脲衍生物被制备出来，并对其作为视黄酸受体相关孤儿受体 α（RORα）激动剂的活性进行了评估。以各种官能团取代的芳基环替代先导化合物 CGP52608（1）中的 3-烯丙基-2-亚氨基-噻唑烷-4-酮部分，提高了 RORα 的激动活性。在所制备的衍生物中，在 RORα 激活测定中，1-甲基-3-（4-苯氧基-苄基）-硫脲（32）的激动活性比 CGP52608 高 2.6 倍。
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