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.
Molecular Weight
253.7300 g/mol
LogP
1.50
TPSA
88.80 Ų
Lipinski RO5
Pass
Therapeutic Areas
Mechanism of Action
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.
2D Structure
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
Rotatable Bonds
4
Heavy Atoms
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.
Frequently Asked Questions
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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