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 …
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 …
(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 …
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
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 …
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 …
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 …
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 …
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 …
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 …
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 …
have been made to find alternative chemotherapeutic agents. In this regard, scientists have …