Cycloguanil

Description

Cycloguanil was first observed in 1951 as a metabolite of the antimalarial drug chlorguanide; it also has shown activity against malaria. Because traditional antimalarials are becoming ineffective against new strains of the malarial protozoan Plasmodium falciparum, renewed efforts are underway to develop cycloguanil into a commercial drug.

The Uses of Cycloguanil

Antimalarial.

Background

Cycloguanil is the active metabolite of proguanil.

Definition

ChEBI: Cycloguanil is a triazine in which a 1,6-dihydro-1,3,5-triazine ring is substituted at N-1 by a 4-chlorophenyl group, at C-2 and -4 by amino groups and at C-6 by gem-dimethyl groups. A dihydrofolate reductase inhibitor, it is a metabolite of the antimalarial drug proguanil. It has a role as an EC 1.5.1.3 (dihydrofolate reductase) inhibitor, an antiinfective agent, an antiparasitic agent, an antimalarial, an antiprotozoal drug and an antifolate.

Metabolism

Not Available