Antimalarial Activity of Highly Coordinative Fused Heterocycles Targeting β-Hematin Crystallization.

ABSTRACT: The β-hematin formation is a unique process adopted by Plasmodium sp. to detoxify free heme and represents a validated target to design new effective antimalarials. Most of the β-hematin inhibitors are mainly based on 4-aminoquinolines, but the parasite has developed diverse defense mechanisms against this type of chemical system. Thus, the identification of other molecular chemical entities targeting the β-hematin formation pathway is highly needed to evade resistance mechanisms associated with 4-aminoquinolines. Herein, we showed that the highly coordinative character can be a useful tool for the rational design of antimalarial agents targeting β-hematin crystallization. From a small library consisting of five compound families with recognized antitrypanosomatid acti

SUBMITTER: Acosta ME 

PROVIDER: S-EPMC8908514 | biostudies-literature | 2022 Mar

REPOSITORIES: biostudies-literature