Role of specific cytochrome P450 isoforms in the conversion of phenoxypropoxybiguanide analogs in human liver microsomes to potent antimalarial dihydrotriazines.

@article{Diaz2008RoleOS,
  title={Role of specific cytochrome P450 isoforms in the conversion of phenoxypropoxybiguanide analogs in human liver microsomes to potent antimalarial dihydrotriazines.},
  author={Damaris S. Diaz and Michael P. Kozar and Kirsten S. Smith and Constance O. Asher and Jason C. Sousa and Guy A. Schiehser and David P. Jacobus and Wilbur K. Milhous and Donald R. Skillman and Todd W. Shearer},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2008},
  volume={36 2},
  pages={380-5}
}
Phenoxypropoxybiguanides, such as PS-15, are antimalarial prodrugs analogous to the relationship of proguanil and its active metabolite cycloguanil. Unlike cycloguanil, however, WR99210, the active metabolite of PS-15, has retained in vitro potency against newly emerging antifolate-resistant malaria parasites. Recently, in vitro metabolism of a new series… CONTINUE READING