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Cycloguanil is a small molecule and the active metabolite of the antimalarial drug proguanil. It acts as a dihydrofolate reductase inhibitor (DHFR), which disrupts folate synthesis in malaria parasites and other susceptible organisms. This mechanism is essential for parasite DNA synthesis and cell division. Cycloguanil is not currently in general use as an antimalarial on its own but remains important due to its role in the efficacy of proguanil-based therapies[1][2][5]. The formation of cycloguanil from proguanil occurs mainly via hepatic metabolism by CYP2C19[3][4].
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