English (United Kingdom)

https://curated-unify.zendy.io/wp-json/zendy-region/v1/featured_content/oa?rat=en

https://curated-unify.zendy.io/wp-json/zendy-region/v1/highlighted_journal/

Global: Zendy Plus annual

Presents the access of premium content as premium feature

Premium Content

Presents the keyphrase highlighting as premium feature

Keyphrase Highlighting

Presents the summarisation as premium feature

Summarisation

Insights

Presents the pdf analysis as premium feature

PDF Analysis

Presents the zaia usage as premium feature

ZAIA

Global: Zendy Plus monthly

Global: Zendy Tools annual

Global: Zendy Tools monthly

Global: Zendy Free Plan

A total of 28 lapachol-related naphthoquinones with four different scaffolds were synthesized and spectroscopically characterized.  In vitro  antiplasmodial activity was assayed against the chloroquine-resistant  Plasmodium falciparum  W2 strain by the parasite lactate dehydrogenase ( p LDH) method. Cytotoxicity against Hep G2A16 cell was determined by the MTT assay. All compounds disclosed higher  in vitro  antiplasmodial activity than lapachol.  Ortho-  and  para -naphthoquinones with a furan ring fused to the quinonoid moiety were more potent than 2-hydroxy-3-(1′-alkenyl)-1,4-naphthoquinones, while  ortho -furanonaphthoquinones were more cytotoxic. Molecular docking to  Plasmodium  targets  Pf cyt  bc1  complex and  Pf DHOD enzyme showed that five out of the 28 naphthoquinones disclosed favorable binding energies. Furanonaphthoquinones endowed with an aryl moiety linked to the furan ring are highlighted as new  in vitro  antiplasmodial lead compounds and warrant further investigation.

Synthesis, SAR, and Docking Studies Disclose 2-Arylfuran-1,4-naphthoquinones as In Vitro Antiplasmodial Hits