Discovery of fast-acting dual-stage antimalarial agents by profiling pyridylvinylquinoline chemical space via copper catalyzed azide-alkyne cycloadditions
G Huang, CM Solano, J Melendez, S Yu-Alfonzo… - European journal of …, 2021 - Elsevier
… Herein, as a continuation of our research on the development of quinoline-based antimalarial
agents, we report the synthesis of a series of 4-pyridylvinylquinoline-triazole conjugates …
agents, we report the synthesis of a series of 4-pyridylvinylquinoline-triazole conjugates …
7-Chloroquinolinotriazoles: Synthesis by the azide–alkyne cycloaddition click chemistry, antimalarial activity, cytotoxicity and SAR studies
GR Pereira, GC Brandão, LM Arantes… - European Journal of …, 2014 - Elsevier
… To prevent the selection of resistant parasites, WHO has recommended the combination
of artemisinins with traditional antimalarial drugs such as lumefantrine, amodiaquine and …
of artemisinins with traditional antimalarial drugs such as lumefantrine, amodiaquine and …
Azide-alkyne cycloaddition en route to 1H-1, 2, 3-triazole-tethered 7-chloroquinoline-isatin chimeras: Synthesis and antimalarial evaluation
… We describe the synthesis and antimalarial activities of 1H-1,2,3-triazole tethered 7-chloroquinoline-isatin
hybrids. Activity against cultured parasites was dependent on the C-5 …
hybrids. Activity against cultured parasites was dependent on the C-5 …
A click chemistry‐based proteomic approach reveals that 1, 2, 4‐trioxolane and artemisinin antimalarials share a common protein alkylation profile
HM Ismail, VE Barton, M Panchana… - Angewandte Chemie …, 2016 - Wiley Online Library
… Concurrently, using both ART-alkyne and azide optimized probes we were able to identify
59 P. falciparum proteins with high confidence that were specifically alkylated by ART pointing …
59 P. falciparum proteins with high confidence that were specifically alkylated by ART pointing …
Antimalarial naphthoquinones. Synthesis via click chemistry, in vitro activity, docking to PfDHODH and SAR of lapachol-based compounds
GC Brandão, FCR Missias, LM Arantes… - European journal of …, 2018 - Elsevier
… antimalarial drugs has been observed as a consequence of genetic mutations and is a serious
setback to antimalarial … terminal alkyne 11 and the organic azide 9 in a convergent route. …
setback to antimalarial … terminal alkyne 11 and the organic azide 9 in a convergent route. …
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
… azide–alkyne cycloaddition, an alternative metal-free pathway has never been reported for
the synthesis of antimalarial … been used before to synthesize antimalarial drug compounds. …
the synthesis of antimalarial … been used before to synthesize antimalarial drug compounds. …
Artemisinin activity-based probes identify multiple molecular targets within the asexual stage of the malaria parasites Plasmodium falciparum 3D7
HM Ismail, V Barton, M Phanchana… - Proceedings of the …, 2016 - National Acad Sciences
… (ART) class of antimalarial drugs, the most important antimalarial drug class in use today, …
, peptide linkers of maximum three carbons were used for our alkyne and azide probes. …
, peptide linkers of maximum three carbons were used for our alkyne and azide probes. …
[HTML][HTML] Antimalarial C-9 oxime derivatives from desmycosin, produced by click chemistry
A Tsutsui, T Hirose, A Ishiyama, M Iwatsuki… - The Journal of …, 2013 - nature.com
… continuing need for new antimalarial drugs that are effective, … and synthesis of antimalarial
agents from microbial metabolites … Moreover, as the discovery of the antimicrobial alkyne-…
agents from microbial metabolites … Moreover, as the discovery of the antimicrobial alkyne-…
Artemisinin–(Iso) quinoline Hybrids by C− H Activation and Click Chemistry: Combating Multidrug‐Resistant Malaria
… drug resistance. ACTs use ART or its derivatives together with one or more other antimalarial
drugs … hand, we linked the alkyne-tagged analogues to biotin azide through click chemistry (…
drugs … hand, we linked the alkyne-tagged analogues to biotin azide through click chemistry (…
Synthesis of triazole-linked chloroquinoline derivatives as novel antimalarial agents
L Taleli - 2013 - scholar.sun.ac.za
… resistance associated with chloroquine analogues. … designed and synthesized as novel
antimalarial agents using the Cu(I)-… -4-amine alkyne precursor and the azides of ethyl and propyl …
antimalarial agents using the Cu(I)-… -4-amine alkyne precursor and the azides of ethyl and propyl …
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