85274-48-2Relevant academic research and scientific papers
Identification and structure activity relationships of quinoline tertiary alcohol modulators of RORγt
Kummer, David A.,Cummings, Maxwell D.,Abad, Marta,Barbay, Joseph,Castro, Glenda,Wolin, Ronald,Kreutter, Kevin D.,Maharoof, Umar,Milligan, Cynthia,Nishimura, Rachel,Pierce, Joan,Schalk-Hihi, Celine,Spurlino, John,Urbanski, Maud,Venkatesan, Hariharan,Wang, Aihua,Woods, Craig,Xue, Xiaohua,Edwards, James P.,Fourie, Anne M.,Leonard, Kristi
, p. 2047 - 2057 (2017/04/10)
A high-throughput screen of the ligand binding domain of the nuclear receptor retinoic acid-related orphan receptor gamma t (RORγt) employing a thermal shift assay yielded a quinoline tertiary alcohol hit. Optimization of the 2-, 3- and 4-positions of the quinoline core using structure-activity relationships and structure-based drug design methods led to the discovery of a series of modulators with improved RORγt inhibitory potency and inverse agonism properties.
Structural Simplification of Bedaquiline: the Discovery of 3-(4-(N,N-Dimethylaminomethyl)phenyl)quinoline-Derived Antitubercular Lead Compounds
He, Chunxian,Preiss, Laura,Wang, Bin,Fu, Lei,Wen, Hui,Zhang, Xiang,Cui, Huaqing,Meier, Thomas,Yin, Dali
supporting information, p. 106 - 119 (2017/02/05)
Bedaquiline (BDQ) is a novel and highly potent last-line antituberculosis drug that was approved by the US FDA in 2013. Owing to its stereo-structural complexity, chemical synthesis and compound optimization are rather difficult and expensive. This study
PHENYL LINKED QUINOLINYL MODULATORS OF RORyt
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Paragraph 0331, (2015/04/21)
The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also
PHENYL LINKED QUINOLINYL MODULATORS OF ROR-GAMMA-T
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Page/Page column 84, (2015/05/05)
The present invention comprises compounds of Formula I. Formula I wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The inve
HETEROARYL LINKED QUINOLINYL MODULATORS OF RORyt
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Paragraph 0254; 0255, (2014/05/07)
The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
Synthesis and 5-Hydroxytryptamine Antagonist Activity of 2-thio>-3-phenylquinoline and Its Analogues
Blackburn, Thomas P.,Cox, Barry,Guildford, Allen J.,Count, David J. Le,Middlemiss, Derek N.,et al.
, p. 2252 - 2259 (2007/10/02)
A series of 2-quinolines substituted at the 3-position with alkyl, aryl, or heteroaryl groups has been prepared in the search for novel and selective 5-HT2 antagonists.The affinity of the compounds for 5-HT1 recep
