cas 58337-16-9, ETHYL 2-ANILINO-4-OXO-4,5-DIHYDRO-3-FURANCARBOXYLATE | Articles data ｜lookchem

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58337-16-9

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Synthesis, design, and structure–activity relationship of the pyrimidone derivatives as novel selective inhibitors of plasmodium falciparum dihydroorotate dehydrogenase
The inhibition of Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) potentially represents a new treatment option for malaria, as P. falciparum relies entirely on a de novo pyrimidine biosynthetic pathway for survival. Herein, we report a series of pyrimidone derivatives as novel inhibitors of PfDHODH. The most potent compound, 26, showed high inhibition activity against PfDHODH (IC50 = 23 nM), with >400-fold species selectivity over human dihydroorotate dehydrogenase (hDHODH). The brand-new inhibitor scaffold targeting PfDHODH reported in this work may lead to the discovery of new antimalarial agents.
Xu, Le,Li, Wenjie,Diao, Yanyan,Sun, Hongxia,Li, Honglin,Zhu, Lili,Zhou, Hongchang,Zhao, Zhenjiang
(2018/06/08)

METHOD FOR TREATING VIRUS INFECTION USING DERIVATIVE OF ANILINE
A method for treating a virus infection in a subject is provided. The method comprising administering to the subject in need an effective amount of a derivative of aniline selected from the group consisting of a compound of formula (I), a pharmaceutically
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Paragraph 0066; 0072

(2015/07/15)

Studies of heterocyclic compounds. VIII. Synthesis, anti-inflammatory and antiallergic activities of N-alkyl-2,3,4,9-tetrahydrofuro[2,3-b]quinoline-3,4-diones and related compounds
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Kuo,Huang,Huang,Cheng,Ling,Wu,Ishii,Nakamura
p. 955 - 963
(2007/10/02)

Drug-induced modifications of the immune response. 12. 4,5-Dihydro-4-oxo-2-(substituted amino)-3-furancarboxylic acids and derivatives as novel antiallergic agents
The synthesis of a series of novel 4,5-dihydro-4-oxo-2-(substituted amino)-3-furancarboxylic acids, salts, esters, and amides is described. The title compounds when tested in the mediator-induced dermal vascular permeability and active anaphylaxis assays in rats demonstrated moderate to potent antiallergic activity. The [2-trans-(4-methyl-phenyl)cyclopropyl]amino analogue 53 emerged as the most active derivative. Thus, when administered intraperitoneally to rate at a dose of 100 mg/kg, it inhibited the action of the mediators serotonin, histamine, and bradykinin by 100%. In the active anaphylaxis assay in rats, compound 30 suppressed the edema by 81% at a dose of 100 mg/kg, following intraperitoneal administration.
Mck,Zazulak,Radov,baer,Steward,Elzer,Kinsolving,Georgiev
p. 1910 - 1918
(2007/10/02)

Synthesis of furoquinolines
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Yazima,Munakata
p. 235 - 243
(2007/10/02)

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Chemical Properties

Melting Point: 118-120°C
Boiling Point: 377.2°Cat760mmHg
Flash Point:182°C
Density: 1.339g/cm³
Vapor Pressure: 6.84E-06mmHg at 25°C
PSA: 64.63000
LogP: 1.54550

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