Discovery of novel N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides as potent RORγt inhibitors

Bioorganic and Medicinal Chemistry

Volumn 22, Issue 2, 2014, Pages 692-702

  Wang, Yonghui ^a   Cai, Wei ^a   Zhang, Guifeng ^a   Yang, Ting ^a   Liu, Qian ^a   Cheng, Yaobang ^a   Zhou, Ling ^a   Ma, Yingli ^a   Cheng, Ziqiang ^a   Lu, Sijie ^a   Zhao, Yong Gang ^a   Zhang, Wei ^a   Xiang, Zhijun ^a   Wang, Shuai ^a   Yang, Liuqing ^a   Wu, Qianqian ^a   Orband Miller, Lisa A ^b   Xu, Yan ^a   Zhang, Jing ^a   Gao, Ruina ^a   Huxdorf, Melanie ^a   Xiang, Jia Ning ^a   Zhong, Zhong ^a   Elliott, John D ^a   Leung, Stewart ^a   Lin, Xichen ^a   more..

^a GLAXOSMITHKLINE   (China)

^b GLAXOSMITHKLINE   (United States)

Author keywords

Multiple sclerosis; Rheumatoid arthritis; ROR t inhibitor; Th17 cell differentiation

Indexed keywords

2 [4 (ETHYLSULFONYL)PHENYL] N [[5 (3 FLUOROBENZOYL) 4 3 (TRIFLUOROMETHYL)PHENYL]THIOPHEN 2 YL]ACETAMIDE; 3 [5 BENZOYL 2 [2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDO]THIAZOL 4 YL]BENZOIC ACID; N (5 BENZOYL 4 PHENYLTHIOPHEN 2 YL) 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [4 (3 CHLOROPHENYL) 5 (2 FLUOROBENZOYL)THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [4 (3 CHLOROPHENYL) 5 (2 FLUOROBENZOYL)THIOPHEN 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [4 (3 CHLOROPHENYL) 5 (3 FLUOROBENZOYL)THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [4 (3 CHLOROPHENYL) 5 (3 FLUOROBENZOYL)THIOPHEN 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [5 (2 CHLOROBENZOYL) 4 (3 CHLOROPHENYL)THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [5 (2 CHLOROBENZOYL) 4 (3 CHLOROPHENYL)THIOPHEN 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [5 (3 CHLOROBENZOYL) 4 (3 CHLOROPHENYL)THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [5 (3 CHLOROBENZOYL) 4 (3 CHLOROPHENYL)THIOPHEN 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [5 (4 CHLOROBENZOYL) 4 (3 CHLOROPHENYL)THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [5 (ARYLCARBONYL)THIAZOL 2 YL]AMIDE; N [5 (ARYLCARBONYL)THIOPHEN 2 YL]AMIDE; N [5 BENZOYL 4 (2 CHLOROPHENYL)THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [5 BENZOYL 4 (3 CHLOROPHENYL)THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [5 BENZOYL 4 (3 CHLOROPHENYL)THIOPHEN 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [5 BENZOYL 4 (3 CYANOPHENYL)THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [5 BENZOYL 4 (3 CYANOPHENYL)THIOPHEN 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [5 BENZOYL 4 (4 CHLOROPHENYL)THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; N [5 BENZOYL 4 [3 [(DIMETHYLAMINO)METHYL]PHENYL]THIAZOL 2 YL] 2 [4 (ETHYLSULFONYL)PHENYL]ACETAMIDE; PROTEIN INHIBITOR; RETINOID RELATED ORPHAN RECEPTOR GAMMA; UNCLASSIFIED DRUG; AMIDE; COLLAGEN; RORC PROTEIN, HUMAN;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTHRITIS; ARTICLE; BINDING AFFINITY; CELL DIFFERENTIATION; CONTROLLED STUDY; DRUG EFFICACY; DRUG POTENCY; EXPERIMENTAL AUTOIMMUNE ENCEPHALOMYELITIS; IN VITRO STUDY; IN VIVO STUDY; MALE; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION; TH17 CELL; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; CHEMICALLY INDUCED; CHEMISTRY; DISEASE MODEL; DOSE RESPONSE; DRUG DEVELOPMENT; DRUG EFFECTS; ENCEPHALOMYELITIS, AUTOIMMUNE, EXPERIMENTAL; HUMAN; ORAL DRUG ADMINISTRATION;

ADMINISTRATION, ORAL; AMIDES; ANIMALS; ARTHRITIS; CELL DIFFERENTIATION; COLLAGEN; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; ENCEPHALOMYELITIS, AUTOIMMUNE, EXPERIMENTAL; HUMANS; MICE; MOLECULAR STRUCTURE; NUCLEAR RECEPTOR SUBFAMILY 1, GROUP F, MEMBER 3; STRUCTURE-ACTIVITY RELATIONSHIP; TH17 CELLS;

EID: 84892366573     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2013.12.021     Document Type: Article

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