Proguanil
Proguanil is a biguanide antimalarial prodrug that is metabolized to its active form cycloguanil, which inhibits plasmodial dihydrofolate reductase, thereby disrupting folate metabolism and DNA synthesis in the malaria parasite. It is used in combination with atovaquone (as Malarone) for both prevention and treatment of malaria, including chloroquine-resistant Plasmodium falciparum infections.
分子量
253.7300 g/mol
LogP
1.50
TPSA
88.80 Ų
Lipinski 五规则
符合
治疗领域
作用机制
Administered as an inactive precursor that is metabolically converted to its active form in the body. This prodrug design improves bioavailability, absorption, or targeted delivery compared to the active compound.
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Administered as an inactive precursor that is metabolically converted to its active form in the body. This prodrug design improves bioavailability, absorption, or targeted delivery compared to the active compound.
二维结构
Cite this structure
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SMILES
CC(C)NC(=N)NC(=N)Nc1ccc(Cl)cc1
InChI
InChI=1S/C11H16ClN5/c1-7(2)15-10(13)17-11(14)16-9-5-3-8(12)4-6-9/h3-7H,1-2H3,(H5,13,14,15,16,17)
Molecular Formula
C11H16ClN5
HBD / HBA
3 / 1
可旋转键数
4
重原子数
17
No targets recorded
Target interaction data is not yet available for this drug.
No interactions recorded
Drug interaction data is not yet available for this compound.
No side effects recorded
Side effect data is not yet available for this drug.
常见问题
Proguanil is a biguanide antimalarial prodrug that is metabolized to its active form cycloguanil, which inhibits plasmodial dihydrofolate reductase, thereby disrupting folate metabolism and DNA synthesis in the malaria parasite. It is used in combination with atovaquone (as Malarone) for both prevention and treatment of malaria, including chloroquine-resistant Plasmodium falciparum infections.
Administered as an inactive precursor that is metabolically converted to its active form in the body. This prodrug design improves bioavailability, absorption, or targeted delivery compared to the active compound.
Yes, Proguanil is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL1377. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 6178111. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.
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