P0049
4-[(7-氯-2-甲氧基-1,5-二氢吡啶并[3,2-b]喹啉-10-基)亚氨]-2,6-二(吡咯烷-1-基甲基)环己-2,5-二烯-1-酮磷酸盐 (1:4)
别名:
76748-86-2
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关于此项目
经验公式（希尔记法）:
C29H32ClN5O2·4H3PO4
化学文摘社编号:
分子量:
910.03
NACRES:
NA.85
PubChem Substance ID:
UNSPSC Code:
51102911
MDL number:
InChI key
YKUQEKXHQFYULM-UHFFFAOYSA-N
SMILES string
OP(O)(O)=O.OP(O)(O)=O.OP(O)(O)=O.OP(O)(O)=O.COc1ccc2nc3cc(Cl)ccc3c(Nc4cc(CN5CCCC5)c(O)c(CN6CCCC6)c4)c2n1
InChI
1S/C29H32ClN5O2.4H3O4P/c1-37-26-9-8-24-28(33-26)27(23-7-6-21(30)16-25(23)32-24)31-22-14-19(17-34-10-2-3-11-34)29(36)20(15-22)18-35-12-4-5-13-35;4*1-5(2,3)4/h6-9,14-16,36H,2-5,10-13,17-18H2,1H3,(H,31,32);4*(H3,1,2,3,4)
form
solid
antibiotic activity spectrum
parasites
mode of action
enzyme | interferes
storage temp.
2-8°C
Application
咯萘啶是一种吖啶衍生物，在中国用于治疗耐药性恶性疟疾。它在体外对喀麦隆恶性疟原虫的活性已有研究。
Biochem/physiol Actions
吡咯烷具有抗疟活性，可与青蒿琥酯联用。其对萘醌和二氢青蒿素有拮抗作用。在体外，吡咯烷可阻止B-血红素形成，并对P-糖蛋白介导的耐药性具有抑制活性。
Other Notes
将容器密闭保存在干燥和通风良好的地方。储存类别 (TRGS 510)：非易燃固体
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Repr. 2
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
Leonardo K Basco et al.
Antimicrobial agents and chemotherapy, 47(4), 1391-1394 (2003-03-26)
The spread of chloroquine-resistant Plasmodium falciparum calls for a constant search for new drugs. The in vitro activity of piperaquine, a new Chinese synthetic drug belonging to the bisquinolines, was evaluated in 103 fresh clinical isolates of P. falciparum in
Matthias Rottmann et al.
Antimicrobial agents and chemotherapy, 64(4) (2020-02-12)
Antimalarial drug resistance in the Plasmodium falciparum parasite poses a constant challenge for drug development. To mitigate this risk, new antimalarial medicines should be developed as fixed-dose combinations. Assessing the pharmacodynamic interactions of potential antimalarial drug combination partners during early
Timothy M E Davis et al.
Antimicrobial agents and chemotherapy, 50(8), 2883-2885 (2006-07-28)
In an in vitro assessment of antimalarial combinations, dihydroartemisinin (DHA) showed no interaction or was mildly antagonistic when combined with piperaquine, pyronaridine, or naphthoquine. Interactions between 4-aminoquinolines and related drugs were also indifferent/antagonistic. The clinical significance of mildly antagonistic DHA
Giorgia Mori et al.
Tuberculosis (Edinburgh, Scotland), 112, 98-109 (2018-09-13)
The search for compounds with biological activity for many diseases is turning increasingly to drug repurposing. In this study, we have focused on the European Union-approved antimalarial pyronaridine which was found to have in vitro activity against Mycobacterium tuberculosis (MIC
Mohamed Abdo Rizk et al.
Scientific reports, 7(1), 12774-12774 (2017-10-19)
In this study, we evaluated the validity of a fluorescence-based assay using SYBR Green I (SG I) stain for screening antibabesial compounds against B. microti in mice. Two different hematocrits (HCTs; 2.5% and 5%) were used. Correlating relative fluorescence units
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