Designing drugs and chemical probes with the dualsteric approach

J Zha, J He, C Wu, M Zhang, X Liu… - Chemical Society Reviews, 2023 - pubs.rsc.org
Traditionally, drugs are monovalent, targeting only one site on the protein surface. This
includes orthosteric and allosteric drugs, which bind the protein at orthosteric and allosteric …

The role of the iron protoporphyrins heme and hematin in the antimalarial activity of endoperoxide drugs

HC Quadros, MCB Silva, DRM Moreira - Pharmaceuticals, 2022 - mdpi.com
Plasmodium has evolved to regulate the levels and oxidative states of iron protoporphyrin IX
(Fe-PPIX). Antimalarial endoperoxides such as 1, 2, 4-trioxane artemisinin and 1, 2, 4 …

Autofluorescent antimalarials by hybridization of artemisinin and coumarin: in vitro/in vivo studies and live-cell imaging

L Herrmann, M Leidenberger, AS de Morais, C Mai… - Chemical …, 2023 - pubs.rsc.org
Malaria is one of our planet's most widespread and deadliest diseases, and there is an ever-
consistent need for new and improved pharmaceuticals. Natural products have been an …

Bestatin analogs-4-quinolinone hybrids as antileishmanial hits: Design, repurposing rational, synthesis, in vitro and in silico studies

AHE Hassan, K Mahmoud, TN Phan… - European Journal of …, 2023 - Elsevier
Amongst different forms of leishmaniasis, visceral leishmaniasis caused by L. donovani is
highly mortal. Identification of new hit compounds might afford new starting points to develop …

Access to Artemisinin–Triazole Antimalarials via Organo-Click Reaction: High In Vitro/In Vivo Activity against Multi-Drug-Resistant Malaria Parasites

L Herrmann, M Leidenberger, HC Quadros, BW Grau… - JACS Au, 2024 - ACS Publications
Malaria is one of the most widespread diseases worldwide. Besides a growing number of
people potentially threatened by malaria, the consistent emergence of resistance against …

The Potentials of Ageratum conyzoides and Other Plants from Asteraceae as an Antiplasmodial and Insecticidal for Malaria Vector: An Article Review

IT Kusman, GW Pradini, IF Ma'ruf… - Infection and Drug …, 2023 - Taylor & Francis
Background Malaria is a life-threatening disease prevalent in tropical and subtropical
regions. Artemisinin combination therapy (ACT) used as an antimalarial treatment has …

The antimalarial activity of 1, 2, 4‐trioxolane/trioxane hybrids and dimers: a review

J Fang, F Song, F Wang - Archiv der Pharmazie, 2022 - Wiley Online Library
Malaria, a mosquito‐borne parasitic infection caused by protozoan parasites belonging to
the genus Plasmodium, is a dangerous disease that contributes to millions of hospital visits …

Characterization of antimalarial activity of artemisinin-based hybrid drugs

HC Quadros, L Herrmann, J Manaranche… - Antimicrobial Agents …, 2024 - Am Soc Microbiol
In response to the spread of artemisinin (ART) resistance, ART-based hybrid drugs were
developed, and their activity profile was characterized against drug-sensitive and drug …

PfMDR1 Transport Rates Assessed in Intact Isolated Plasmodium falciparum Digestive Vacuoles Reflect Functional Drug Resistance Relationship with pfmdr1 …

N Simon, C Voigtländer, B Kappes, P Rohrbach… - Pharmaceuticals, 2022 - mdpi.com
Drug resistance often emerges from mutations in solute transporters. Single amino acid
exchanges may alter functionality of transporters with 'de novo'ability to transport drugs away …

In vitro and in vivo antiplasmodial activity of a synthetic dihydroartemisinin–eosin B hybrid

HK Askarani, A Tahghighi, M Ahmadpoor… - Naunyn-Schmiedeberg's …, 2024 - Springer
With the inexorable prevalence and spread of drug-resistant malaria strains, many efforts
have been made to find alternative chemotherapeutic agents. In this regard, scientists have …