Discovery of N-(4-aryl-5-aryloxy-thiazol-2-yl)-amides as potent RORγt inverse agonists

Bioorganic and Medicinal Chemistry

Volumn 23, Issue 17, 2015, Pages 5293-5302

  Wang, Yonghui ^a   Yang, Ting ^b   Liu, Qian ^b   Ma, Yingli ^b   Yang, Liuqing ^b   Zhou, Ling ^b   Xiang, Zhijun ^b   Cheng, Ziqiang ^b   Lu, Sijie ^b   Orband Miller, Lisa A ^b   Zhang, Wei ^b   Wu, Qianqian ^b   Zhang, Kathleen ^b   Li, Yi ^b   Xiang, Jia Ning ^b   Elliott, John D ^b   Leung, Stewart ^b   Ren, Feng ^b   Lin, Xichen ^b  

^a FUDAN UNIVERSITY   (China)

^b GLAXOSMITHKLINE   (China)

Author keywords

Crystal structure; ROR t inverse agonists; Th17 cell differentiation; Thiazole ether amides

Indexed keywords

2 [4 (ETHYLSULFONYL)PHENYL]N (4 PHENYL 5 [[4 (TRIFLUOROMETHYL)PHENYL]OXY] 1,3 THIAZOL 2 YL)ACETAMIDE; 2 [4 (ETHYLSULFONYL)PHENYL]N (5 [[2 (METHYLOXY)PHENYL]OXY] 4 PHENYL 1,3 THIAZOL 2 YL)ACETAMIDE; 2 [4 (ETHYLSULFONYL)PHENYL]N (5 [[4 (METHYLOXY)PHENYL]OXY] 4 PHENYL 1,3 THIAZOL 2 YL)ACETAMIDE; 2 [4 (ETHYLSULFONYL)PHENYL]N [4 PHENYL 5 (PHENYLMETHYL) 1,3 THIAZOL 2 YL]ACETAMIDE; 2 [4 (ETHYLSULFONYL)PHENYL]N [4 PHENYL 5 (PHENYLOXY) 1,3 THIAZOL 2 YL]ACETAMIDE; N (4 ARYL 5 PHENYL THIAZOL 2 YL)AMIDE DERIVATIVE; N (4,5 DIPHENYL 1,3 THIAZOL 2 YL) 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [4 (2,5 DICHLOROPHENYL) 1,3 THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [4 (2,5 DICHLOROPHENYL) 5 ETHYL 1,3 THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [4 (2,5 DICHLOROPHENYL) 5 METHYL 1,3 THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [4 (2,5 DICHLOROPHENYL) 5 PHENYL 1,3 THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [4 (3 CHLOROPHENYL) 5 PHENOXYTHIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [4 (3 CHLOROPHENYL) 5 [2 (TRIFLUOROMETHYL)PHENOXY]THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [4 (3 CYANOPHENYL) 5 [2 (TRIFLUOROMETHYL)PHENOXY]THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [4 (4 CHLOROPHENYL) 5 (PHENYLOXY) 1,3 THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [4 [3 [(DIMETHYLAMINO)METHYL]PHENYL] 5 [2 (TRIFLUOROMETHYL)PHENOXY]THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDETRIFLUOROACETATE; N [5 [(2 CHLOROPHENYL)OXY] 4 PHENYL 1,3 THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [5 [(4 CHLOROPHENYL)OXY] 4 PHENYL 1,3 THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [5 [2 CHLORO 4 (TRIFLUOROMETHYL)PHENOXY] 4 (3 CYANOPHENYL)THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [5 [4 CHLORO 2 (TRIFLUOROMETHYL)PHENOXY] 4 (3 CYANOPHENYL)THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; PROTEIN INHIBITOR; RETINOID RELATED ORPHAN RECEPTOR GAMMA; UNCLASSIFIED DRUG; AMIDE; THIAZOLE DERIVATIVE;

ANIMAL CELL; ARTICLE; CELL DIFFERENTIATION; DRUG BINDING; DRUG CLEARANCE; DRUG IDENTIFICATION; DRUG POTENCY; DRUG STABILITY; DRUG STRUCTURE; DRUG SYNTHESIS; EC50; IC50; IN VITRO STUDY; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION; AGONISTS; ANIMAL; CELL CULTURE; CHEMISTRY; CYTOLOGY; DRUG EFFECTS; HUMAN; INVERSE AGONISM; METABOLISM; MOLECULAR DOCKING; TH17 CELL;

AMIDES; ANIMALS; CELL DIFFERENTIATION; CELLS, CULTURED; DRUG INVERSE AGONISM; HUMANS; MICE; MOLECULAR DOCKING SIMULATION; NUCLEAR RECEPTOR SUBFAMILY 1, GROUP F, MEMBER 3; TH17 CELLS; THIAZOLES;

EID: 84946495603     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2015.07.068     Document Type: Article

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