N-methylthioureas as new agonists of retinoic acid receptor-related orphan receptor

Y Park, S Hong, M Lee, H Jung, WJ Cho, EJ Kim…

Index: Park, Yohan; Hong, Suckchang; Lee, Myungmo; Jung, Hyojun; Cho, Won-Jea; Kim, Eun-Jin; Son, Ho-Young; Lee, Mi-Ock; Park, Hyeung-Geun Archives of Pharmacal Research, 2012 , vol. 35, # 8 p. 1393 - 1401

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Citation Number: 4

Abstract

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 ...