Herrmann L, Leidenberger M, Quadros HC, Grau B, Hampel F, Friedrich O, Moreira DR, Kappes B, Tsogoeva S (2024)
Publication Type: Journal article
Publication year: 2024
Book Volume: 4
Pages Range: 951-957
Journal Issue: 3
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 established antimalarial pharmaceuticals leads to an urge toward new antimalarial drugs. Hybridization of two chemically diverse compounds into a new bioactive product is a successful concept to improve the properties of a hybrid drug relative to the parent compounds and also to overcome multidrug resistance. 1,2,3-Triazoles are a significant pharmacophore system among nitrogen-containing heterocycles with various applications, such as antiviral, antimalarial, antibacterial, and anticancer agents. Several marketed drugs possess these versatile moieties, which are used in a wide range of medical indications. While the synthesis of hybrid compounds containing a 1,2,3-triazole unit was described using Cu- and Ru-catalyzed azide-alkyne cycloaddition, an alternative metal-free pathway has never been reported for the synthesis of antimalarial hybrids. However, a metal-free pathway is a green method that allows toxic and expensive metals to be replaced with an organocatalyst. Herein, we present the synthesis of new artemisinin-triazole antimalarial hybrids via a facile Ramachary-Bressy-Wang organocatalyzed azide-carbonyl [3 + 2] cycloaddition (organo-click) reaction. The prepared new hybrid compounds are highly potent in vitro against chloroquine (CQ)-resistant and multi-drug-resistant Plasmodium falciparum strains (IC
APA:
Herrmann, L., Leidenberger, M., Quadros, H.C., Grau, B., Hampel, F., Friedrich, O.,... Tsogoeva, S. (2024). Access to Artemisinin-Triazole Antimalarials via Organo-Click Reaction: High In Vitro/In Vivo Activity against Multi-Drug-Resistant Malaria Parasites. JACS Au, 4(3), 951-957. https://doi.org/10.1021/jacsau.3c00716
MLA:
Herrmann, Lars, et al. "Access to Artemisinin-Triazole Antimalarials via Organo-Click Reaction: High In Vitro/In Vivo Activity against Multi-Drug-Resistant Malaria Parasites." JACS Au 4.3 (2024): 951-957.
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