title: N-methylthioureas as new agonists of retinoic acid receptor-related orphan receptor.
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.
authors.affiliation: College of Pharmacy, Inje University, 607 Obang-dong, Gimhae, Gyeongnam, 621-749, Korea.
authors.forename: Yohan
authors.initials: Y
authors.lastname: Park
authors.forename: Suckchang
authors.initials: S
authors.lastname: Hong
authors.forename: Myungmo
authors.initials: M
authors.lastname: Lee
authors.forename: Hyojun
authors.initials: H
authors.lastname: Jung
authors.forename: Won-Jea
authors.initials: WJ
authors.lastname: Cho
authors.forename: Eun-Jin
authors.initials: EJ
authors.lastname: Kim
authors.forename: Ho-Young
authors.initials: HY
authors.lastname: Son
authors.forename: Mi-Ock
authors.initials: MO
authors.lastname: Lee
authors.forename: Hyeung-Geun
authors.initials: HG
authors.lastname: Park
mesh_terms: D056945:Hep G2 Cells; D006801:Humans; D057094:Nuclear Receptor Subfamily 1, Group F, Member 1 / Q000819:agonists*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry / Q000494:pharmacology*; D013882:Thiosemicarbazones / Q000737:chemistry / Q000494:pharmacology*; D013890:Thiourea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D057094:Nuclear Receptor Subfamily 1, Group F, Member 1; C539738:RORA protein, human; D013844:Thiazoles; D013882:Thiosemicarbazones; C002267:N-methylthiourea; C092451:CGP 52608; D013890:Thiourea