proguanil

Ligand id: 9676

Name: proguanil

Structure and Physico-chemical Properties

2D Structure
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Calculated Physico-chemical Properties
Hydrogen bond acceptors 5
Hydrogen bond donors 3
Rotatable bonds 4
Topological polar surface area 88.79
Molecular weight 253.11
XLogP 1.84
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Proguanil is used in combination with atovaquone in both the treatment of uncomplicated malaria caused by P. falciparum and in malaria prophylaxis [1].
Proguanil is on the World Health Organisation's List of Essential Medicines. Click here to access the pdf version of the WHO's 21st Essential Medicines list (2019).
Mechanism Of Action and Pharmacodynamic Effects
Cycloguanil, the active metabolite of proguanil, is an inhibitor of Plasmodium dihydrofolate reductase (DHFR). Proguanil has a different mechanism of action when used in combination with atovaquone, with the prodrug having synergistic activity, leading to enhanced collapse of the mitochondrial membrane potential [2].
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