61707-79-7Relevant academic research and scientific papers
Tetrazole substituted quinolinone derivative and preparation method and application thereof
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, (2020/08/25)
The invention discloses a tetrazole substituted quinolinone derivative and a preparation method and application thereof, and belongs to the technical field of organic compound preparation. The structure of the compound is shown as a formula (I) or pharmaceutically acceptable salt thereof, and in the formula, R1 is tetrazole, R2 is a hydrogen atom or a halogen atom, and R3 is a hydrogen atom, a halogen atom, a nitro group or a trifluoromethyl group. The product disclosed by the invention is a high-efficiency aldose reductase inhibitor with excellent membrane permeability, and the in-vivo availability of the inhibitor can be improved, so that the effect of treating diabetic complications is achieved.
Quinolone-based compounds, formulations, and uses thereof
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Page/Page column 102; 110, (2018/07/02)
Provided herein are quinolone-based compounds that can be used for treatment and/or prevention of malaria and formulations thereof. Also provided herein are methods of treating and/or preventing malaria in a subject by administering a quinolone-based compound or formulation thereof provided herein.
ICI 56,780 optimization: Structure-activity relationship studies of 7-(2-phenoxyethoxy)-4(1H)-quinolones with antimalarial activity
Maignan, Jordany R.,Lichorowic, Cynthia L.,Giarrusso, James,Blake, Lynn D.,Casandra, Debora,Mutka, Tina S.,LaCrue, Alexis N.,Burrows, Jeremy N.,Willis, Paul A.,Kyle, Dennis E.,Manetsch, Roman
, p. 6943 - 6960 (2016/08/05)
Though malaria mortality rates are down 48% globally since 2000, reported occurrences of resistance against current therapeutics threaten to reverse that progress. Recently, antimalarials that were once considered unsuitable therapeutic agents have been revisited to improve physicochemical properties and efficacy required for selection as a drug candidate. One such compound is 4(1H)-quinolone ICI 56,780, which is known to be a causal prophylactic that also displays blood schizonticidal activity against P. berghei. Rapid induction of parasite resistance, however, stalled its further development. We have completed a full structure-activity relationship study on 4(1H)-quinolones, focusing on the reduction of cross-resistance with atovaquone for activity against the clinical isolates W2 and TM90-C2B, as well as the improvement of microsomal stability. These studies revealed several frontrunner compounds with superb in vivo antimalarial activity. The best compounds were found to be curative with all mice surviving a Plasmodium berghei infection after 30 days.
A synthesis of 4-quinolone-3-carboxylic acids via pyrolysis of N- aryldioxopyrrolines
Mohri, Kunihiko,Kanie, Akihiko,Horiguchi, Yoshie,Isobe, Kimiaki
, p. 2377 - 2384 (2007/10/03)
A synthesis of 4-quinolone-3-carboxylic acids (8) was achieved by pyrolysis of 4,5-dimethoxycarbonyl-1-aryl-1H-pyrrole-2,3-diones (3) followed by selective demethoxycarbonylation of the resulting 2,3-dimethoxycarbonyl-4- quinolones (4) in excellent overall yields.
A convenient approach to 1,4-dihydro-4-oxo-3-quinoline carboxylates by electro-oxidative formation of enamine moiety
Torii, Sigeni,Okumoto, Hiroshi,Xu, Long He
, p. 665 - 674 (2007/10/02)
A practical synthetic approach to the drugs of current interest, 1,4-dihydro-4-oxo-quinoline-3-carboxylic acids, has been accomplished through the electro-oxidative formation of double bond adjacent to the nitrogen atom. The efficiency was shown by the in
