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.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Hep G2 Cells
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Humans
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Nuclear Receptor Subfamily 1, Group F, Member 1 / agonists*
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Structure-Activity Relationship
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Thiazoles / chemistry
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Thiazoles / pharmacology*
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Thiosemicarbazones / chemistry
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Thiosemicarbazones / pharmacology*
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Thiourea / analogs & derivatives*
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Thiourea / chemical synthesis
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Thiourea / chemistry
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Thiourea / pharmacology
Substances
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Nuclear Receptor Subfamily 1, Group F, Member 1
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RORA protein, human
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Thiazoles
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Thiosemicarbazones
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N-methylthiourea
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CGP 52608
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Thiourea