NOVEL THIOUREA DERIVATIVES AS ACTIVATORS OF RORalpha AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
Provided is a compound activating RORα gene, particularly a JC1 compound containing CGP52608 thiazolidinedione as a lead substance, and a pharmaceutically acceptable salt thereof. The compound is a lipid accumulation inhibitor and applicable to the treatment of metabolic diseases or inflammatory diseases.
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Paragraph 0069; 0070; 0135; 0136
(2018/11/02)
N-methylthioureas as new agonists of retinoic acid receptor-related orphan receptor
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.
Park, Yohan,Hong, Suckchang,Lee, Myungmo,Jung, Hyojun,Cho, Won-Jea,Kim, Eun-Jin,Son, Ho-Young,Lee, Mi-Ock,Park, Hyeung-Geun
p. 1393 - 1401
(2013/01/15)
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