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KMID : 0043320120350081393
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Archives of Pharmacal Research
2012 Volume.35 No. 8 p.1393 ~ p.1401
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N-methylthioureas as new agonists of retinoic acid receptor-related orphan receptor
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Park Yo-Han
Hong Suck-Chang
Lee Myung-Mo
Jung Hyo-Jun
Cho Won-Jea
Kim Eun-Jin
Son Ho-Young
Lee Mi-Ock
Park Hyeung-Geun
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Abstract
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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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KEYWORD
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Thiourea derivatives, Agonists, Retinoid acid receptor-related orphan receptor α, CGP52608
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