Quantum Chemical Lipophilicities of Antimalarial Drugs in Relation to Terminal Half-Life.

ABSTRACT: According to the WHO, artemisinin-based combination therapies (ACTs) have been integral to the recent reduction in deaths due to Plasmodium falciparum malaria. ACT-resistant strains are an emerging problem and have evolved altered developmental stages, reducing exposure of the most susceptible stages to artemisinin drugs in popular ACTs. Lipophilicity, log K ow, is a guide in understanding and predicting pharmacokinetic properties such as terminal half-life which alters drug exposure. Consistent log K ow values are not necessarily available for artemisinin derivatives designed to extend terminal half-life, increase bioavailability, and reduce neurotoxicity. For other drugs used in ACTs, an assortment of experimental and computational log K ow values are available in the literature and in s

SUBMITTER: Alia JD 

PROVIDER: S-EPMC7114756 | biostudies-literature | 2020 Mar

REPOSITORIES: biostudies-literature