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  3. Antimalarial agent 25

Antimalarial agent 25 is an orally active 1,4-naphthoquinones derivative with antimalarial activity. Antimalarial agent 25 shows cytotoxicity against P. falciparum. Antimalarial agent 25 inhibits P. burghei induced parasitemia in vivo.

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Antimalarial agent 25 Chemical Structure

Antimalarial agent 25 Chemical Structure

CAS No. : 2944456-41-9

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Description

Antimalarial agent 25 is an orally active 1,4-naphthoquinones derivative with antimalarial activity. Antimalarial agent 25 shows cytotoxicity against P. falciparum. Antimalarial agent 25 inhibits P. burghei induced parasitemia in vivo[1].

In Vitro

Antimalarial agent 25 (compound 8) inhibits P. falciparum with IC50 of 4.2 μM, while shows CC50 on mammalian cells with CC50s of 289.2 μM (HepG2), and 400.6 μM (Vero), respectively[1].
Antimalarial agent 25 (compound 8) (15.62-1000 μM; 2 h) shows hemolytic activity below 40% at concentrations from 15.6 to 250 μM in uninfected human erythrocytes[1].
Antimalarial agent 25 (compound 8) (30-0.411 μg/mL; 48 h) causes morphological changes such as complete cytoplasmic degradation and loss of membrane integrity in the W2 strain of P. falciparum[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: W2 strain of P. falciparum (CQ-resistant)
Concentration: 30 - 0.411 μg/mL
Incubation Time: 48 h
Result: Presented completely degraded cytoplasm with loss of membrane integrity, dense cytoplasm with some possible undefined organelles in degenerating stage, and a possible deteriorated food vacuole.
In Vivo

Antimalarial agent 25 (compound 8) (30 mg/kg; po; once daily for 4 consecutive days) shows antimalarial activity in female albino swiss mice[1]. Antimalarial agent 25 (300 mg/kg; po; single dose) shows no significant pathological changes and histopathological damage in female mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mice infected with Plasmodium berghei ANKA[1]
Dosage: 30 mg/kg
Administration: Oral administration; for 4 consecutive days
Result: Partly reduced P. berghei infection.
Parasitemia decreased by 33% on the seventh day (post-treatment).
Molecular Weight

374.39

Formula

C21H18N4O3

CAS No.
SMILES

COC1=CC=C(C=C1)C2=CN(N=N2)CCNC3=CC(C4=CC=CC=C4C3=O)=O

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References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Antimalarial agent 25
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HY-149938
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