84906-81-0Relevant articles and documents
Quinoline carboxamide core moiety-based compounds inhibit P. falciparum falcipain-2: Design, synthesis and antimalarial efficacy studies
Singh, Anju,Kalamuddin, Md,Maqbool, Mudasir,Mohmmed, Asif,Malhotra, Pawan,Hoda, Nasimul
, (2020/12/07)
Targeting Falcipain-2 (FP2) for the development of antimalarials is a promising and established concept in antimalarial drug discovery and development. FP2, a member of papain-family cysteine protease of the malaria parasite Plasmodium falciparum holds an important role in hemoglobin degradation pathway. A new series of quinoline carboxamide-based compounds was designed, synthesized and evaluated for antimalarial activity. We integrated molecular hybridization strategy with in-silico drug design to develop FP2 inhibitors. In-vitro results of FP2 inhibition by Qs17, Qs18, Qs20 and Qs21 were found to be in low micromolar range with IC50 4.78, 7.37, 2.14 and 2.64 μM, respectively. Among the 25 synthesized compounds, four compounds showed significant antimalarial activities. These compounds also depicted morphological and food-vacuole abnormalities much better than that of E-64, an established FP2 inhibitor. Overall these aromatic substituted quinoline carboxamides can serve as promising leads for the development of novel antimalarial agents.
Preparation method of 2-hydroxy-4-carboxylquinoline
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Paragraph 0021; 0023, (2018/06/26)
The invention belongs to the technical field of chemical synthesis and in particular relates to a production preparation method of a dibucaine hydrochloride intermediate 2-hydroxy-4-carboxylquinoline.The method comprises the following steps: (1) putting glacial acetic acid into a reaction kettle; while stirring, adding isatin, malonic acid and sodium acetate; (2) heating the solution in step (1)and raising the temperature until the solution is reflowed; after reflowing, cooling to room temperature; (3) decompressing and evaporating materials in step (2) to remove the glacial acetic acid (which is recycled); (4) adding de-ionized water into the materials which are subjected to evaporation to remove the glacial acetic acid in step (3), and stirring and crystallizing; after finishing crystallization, spinning and filtering; eluting with the glacial acetic acid and then eluting with methanol; drying a wet product to obtain the 2-hydroxy-4-carboxylquinoline. The synthesis method providedby the invention adopts a one-spoon stewing technology to obtain a target product, so that the operation is simplified, the production period is shortened and the production cost is reduced; the obtained product has high purity and high yield and is suitable for large-scale production.
ANTI-MALARIAL AGENTS
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Page/Page column 44, (2013/11/05)
The present invention relates to a novel class of quinolone-4-carboxamide Pf3D7 inhibitors of general formula (I) (Formula (I)) wherein R1, R2, R3, R4, R5, R6, R7, R8 and X are as defined herein, to their use in medicine, and in the treatment of malaria in particular, to compositions containing them, to processes for their preparation and to intermediates used in such processes.
