Abstract
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.
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Park, Y., Hong, S., Lee, M. et al. N-methylthioureas as new agonists of retinoic acid receptor-related orphan receptor. Arch. Pharm. Res. 35, 1393–1401 (2012). https://doi.org/10.1007/s12272-012-0809-0
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DOI: https://doi.org/10.1007/s12272-012-0809-0