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
MDL编号:
UNSPSC代码:
51102911
PubChem化学物质编号:
NACRES:
NA.85
表单
solid
抗生素抗菌谱
parasites
作用机制
enzyme | interferes
储存温度
2-8°C
SMILES字符串
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)
InChI key
YKUQEKXHQFYULM-UHFFFAOYSA-N
应用
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。
生化/生理作用
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。
其他说明
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
警示用语：
Warning
危险声明
危险分类
Acute Tox. 4 Oral - Repr. 2
储存分类代码
11 - Combustible Solids
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
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
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
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
Mahmoud AbouLaila et al.
Pathogens (Basel, Switzerland), 9(3) (2020-03-04)
The present experimental study was conducted for the assessment of the efficacy of in vitro inhibition of myrrh oil on the propagation of Babesia bovis, B. divergens, B. bigemina, Theileria equi, and B. caballi and in vivo efficacy on B.
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