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

ME Acosta, L Gotopo, N Gamboa, JR Rodrigues… - ACS …, 2022 - ACS Publications
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 …

Identification and Mechanistic Evaluation of Hemozoin-Inhibiting Triarylimidazoles Active against Plasmodium falciparum

KJ Wicht, JM Combrinck, PJ Smith… - ACS Medicinal …, 2017 - ACS Publications
In a previous study, target based screening was carried out for inhibitors of β-hematin
(synthetic hemozoin) formation, and a series of triarylimidazoles were identified as active …

Deconstructing Quinoline‐Class Antimalarials to Identify Fundamental Physicochemical Properties of Beta‐Hematin Crystal Growth Inhibitors

KN Olafson, TQ Nguyen, PG Vekilov… - … –A European Journal, 2017 - Wiley Online Library
A versatile approach to control crystallization involves the use of modifiers, which are
additives that interact with crystal surfaces and alter their growth rates. Elucidating a …

Potent antimalarial activity of two arenes linked with triamine designed to have multiple interactions with heme

Y Sakata, K Yabunaka, Y Kobayashi… - ACS Medicinal …, 2018 - ACS Publications
Based on the idea that compounds designed to exhibit high affinity for heme would block
hemozoin formation, a critical heme-detoxification process for malarial parasites, we …

[HTML][HTML] Identification of β-hematin inhibitors in a high-throughput screening effort reveals scaffolds with in vitro antimalarial activity

RD Sandlin, KY Fong, KJ Wicht, HM Carrell… - International Journal for …, 2014 - Elsevier
The emergence of drug resistant strains of Plasmodium spp. creates a critical need for the
development of novel antimalarials. Formation of hemozoin, a crystalline heme …

Synthesis and in silico ADME/Tox profiling studies of heterocyclic hybrids based on chloroquine scaffolds with potential antimalarial activity

H Ramírez, E Fernandez-Moreira, JR Rodrigues… - Parasitology …, 2022 - Springer
A series of heterocyclic chloroquine hybrids containing either a β-phenethylamine fragment
or a 2-aminoindane moiety were synthesized and screened in vitro as inhibitors of β …

Antimalarial hemozoin inhibitors (β-hematin formation inhibition): latest updates

JN Cruz, SN Mali - Combinatorial Chemistry & High …, 2022 - ingentaconnect.com
Malaria is a preventable and curable disease known to be caused by the parasitic infection
of Plasmodium spp., which is transmitted through the bites of infected female Anopheles …

Insights into structural and physicochemical properties required for β-hematin inhibition of privileged triarylimidazoles

CGL Veale, J Jayram, S Naidoo, D Laming… - RSC Medicinal …, 2020 - pubs.rsc.org
In this study, we investigated a series of triarylimidazoles, in an effort to elucidate critical
SAR information pertaining to their anti-plasmodial and β-hematin inhibitory activity. Our …

[HTML][HTML] Identification of β-hematin inhibitors in the MMV Malaria Box

KY Fong, RD Sandlin, DW Wright - International Journal for Parasitology …, 2015 - Elsevier
Abstract The Malaria Box, assembled by the Medicines for Malaria Venture, is a set of 400
structurally diverse, commercially available compounds with demonstrated activity against …

Heme detoxification in the malaria parasite: A target for antimalarial drug development

KA de Villiers, TJ Egan - Accounts of chemical research, 2021 - ACS Publications
Conspectus Over the last century, malaria deaths have decreased by more than 85%.
Nonetheless, there were 405 000 deaths in 2018, mostly resulting from Plasmodium …