- Synthetic method of 8-(trifluoromethyl)quinoline-3-carboxylate
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The invention provides a synthetic method of 8-(trifluoromethyl)quinoline-3-carboxylate. The synthetic method comprises the following steps: reacting 2-(trifluoromethyl)aniline serving as a starting raw material to obtain 8-(trifluoromethyl)quinoline-3-ethyl ester carboxylate; lastly, hydrolyzing the 8-(trifluoromethyl)quinoline-3-ethyl ester carboxylate in an alkaline environment to obtain 8-(trifluoromethyl)quinoline-3-carboxylate. According to the synthetic method of the 8-(trifluoromethyl)quinoline-3-carboxylate provided by the invention, a synthetic route taking 2-(trifluoromethyl)anilineas a raw material is provided. The synthetic method has the advantages of simple synthetic route, reasonable process selection, low raw material cost, adoption of simple and readily-available raw materials, convenience in operation and post-treatment, high total yield, no use of any highly-toxic reagent, easiness in amplification, realization of large-scale production and the like.
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- Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRβ and low blood-brain penetration
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A series of quinoline-3-carboxamide containing sulfones was prepared and found to have good binding affinity for LXRβ and moderate binding selectivity over LXRα. The 8-Cl quinoline analog 33 with a high TPSA score, displayed 34-fold binding selectivity for LXRβ over LXRα (LXRβ IC50 = 16 nM), good activity for inducing ABCA1 gene expression in a THP macrophage cell line, desired weak potency in the LXRα Gal4 functional assay, and low blood-brain barrier penetration in rat.
- Hu, Baihua,Bernotas, Ron,Unwalla, Rayomand,Collini, Michael,Quinet, Elaine,Feingold, Irene,Goos-Nilsson, Annika,Wilhelmsson, Anna,Nambi, Ponnal,Evans, Mark,Wrobel, Jay
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scheme or table
p. 689 - 693
(2010/06/14)
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- Design and synthesis of some new quinoline-3-carbohydrazone derivatives as potential antimycobacterial agents
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A series of 26 new quinoline derivatives carrying active pharmacophores has been synthesized and evaluated for their in vitro antituberculosis activity against Mycobacterium tuberculosis H37Rv (MTB), Mycobacterium smegmatis (MC2), and Mycobacterium fortuitum following the broth micro dilution assay method. Compounds 13e, 13i, 13k, 14a, 14c, 14i, and 14k exhibited significant minimum inhibition concentrations, when compared with first line drugs isoniazid (INH) and rifampicin (RIF) and could be ideally suited for further modifications to obtain more efficacious compounds in the fight against multi-drug resistant tuberculosis.
- Eswaran, Sumesh,Adhikari, Airody Vasudeva,Pal, Nishith K.,Chowdhury, Imran H.
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supporting information; experimental part
p. 1040 - 1044
(2010/06/14)
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- QUINOLINE DERIVATIVES AS CASPASE-3 INHIBITOR, PREPARATION PROCESS FOR THE SAME AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Provided is a quinoline derivative represented by the following Formula (1) for use in treating a caspase- mediated disease by inhibition of caspase-3 activity. Further provided are a method for preparing the quinoline derivative or a pharmaceutically acceptable salt thereof and a pharmaceutical composition containing the same.
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Page/Page column 67-69
(2008/12/07)
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- Quinolines useful in treating cardiovascular disease
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This invention provides compounds of formula I that are useful in the treatment or inhibition of LXR mediated diseases.
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Page/Page column 28
(2008/06/13)
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- Synthesis and SAR of bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors
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Potent and selective bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors were synthesized by a novel convergent route. Selectivity and efficacy versus MMPs and TACE could be controlled by appropriate substitution on the scaffolds and by variation of the P1′ group. Select compounds were found to be effective in in vivo models of arthritis.
- Zask,Gu,Albright,Du,Hogan,Levin,Chen,Killar,Sung,DiJoseph,Sharr,Roth,Skala,Jin,Cowling,Mohler,Barone,Black,March,Skotnicki
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p. 1487 - 1490
(2007/10/03)
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