Antimalarial drugs

Sawyer, Benjamin J.; Khan, Md Imdadul H.; Le, Hoang V.

doi:10.1016/b978-0-323-90575-6.00007-7

Cited by 2 publications

(1 citation statement)

References 213 publications

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“…For example, quinine, which was used for centuries to treat malaria, was isolated from the bark of the cinchona tree. Artemisinin, another highly effective antimalarial drug, was discovered in the 1970s in a traditional Chinese herbal medicine (Dias et al, 2012, Sawyer et al, 2023and Sinha et al, 2023. The discovery and development of safe and e cacious antimalarial medications, especially transmission-blocking ones, are essential to combating drug resistance and malaria transmission (Wadi, 2018).…”

Section: Introductionmentioning

confidence: 99%

Stage -Specific Antimalarial Activity of Alkaloidal Fractions of the Avicennia africana P. Beauv. (Avicenniaceae) Leaf Extract

Ahmed,

Ackah-Armah,

Ghartey-Kwansah

et al. 2024

Preprint

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Background The global call for malaria eradication rested on finding drugs that not only act against asexual but also sexual forms of the parasite. The drawbacks in disease control and prevention due to drug-resistant clones of the parasite piqued our interest in exploring for alternative antimalarial drugs from the mangrove resources. Aims This study evaluates the stage-specific anti-malarial and cytotoxic activities of the fractions of crude alkaloidal extracts from Avicennia africana leaves. Methods The crude and alkaloidal extracts (AAA and AAQ) from A. africana were fractionated using column chromatography and further analysed using GC-mass spectroscopy. The fractions were then tested for antimalarial activity against the trophozoites, schizonts, and gametocyte stages of chloroquine-sensitive strains of 3D7 P. falciparum using the SYBR Green 1 assay. The cytotoxic effects of the fractions were evaluated using the MTT-based assay. Results The fractions AAA1-AAA5 and AAQ1-AAQ5 produced promising trophozoitocidal activities with an IC50 value range of 0.399–45.690 µg/mL, with the artesunate (ref drug) yielding 0.09x103 µg/mL. The schizonticidal and gametocytocidal activities of selected fractions demonstrated high potency with IC50s of 0.622–18.820 µg/mL against artesunate (ref drugs) with 1.800x10-3 and 5.100x10-3 µg/mL, respectively. The cytotoxic effect of fractions produced CC50 that was higher than 100 µg/mL with negligible cytotoxicity on erythrocytes and SI that ranged from 2.189 to 280.899. The major compounds identified in fractions AAA1, AAQ1, and AAQ2 were 8-carbomoylquinoline, razoxane, and dexrazoxane, respectively. Conclusion The fractions exhibited promising trophozoitocidal, schizonticidal, and gametocytocidal effects with no significant cytotoxic effects on RBCs. Quinoline-based alkaloids and iron chelators in this plant are implicated as possible lead-compound transmission blockers of the parasite.

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Section: Introductionmentioning

confidence: 99%

Stage -Specific Antimalarial Activity of Alkaloidal Fractions of the Avicennia africana P. Beauv. (Avicenniaceae) Leaf Extract

Ahmed,

Ackah-Armah,

Ghartey-Kwansah

et al. 2024

Preprint

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Dearomative Functionalization of Activated Quinolines: Transfer Hydrogenation/Cycloaddition Cascade to Construct α‐Tertiary Amines

Yadav,

Kant,

Rao Kuram

2024

Adv Synth Catal

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Cascade dearomative functionalization is a robust protocol to convert flat arenes into medicinally relevant three‐dimensional architectures with added new functionality. Herein, a dearomative cycloaddition protocol for synthesizing tetrahydroquinoline‐embedded α‐tertiary amine scaffolds has been developed employing quinolinium salts and sulfonyl azides under metal‐free conditions. An underexplored and mechanistically distinct pathway is unveiled, creating quaternary‐center‐bearing amine skeletons by an amine group migration during the transfer hydrogenation and cycloaddition cascade reaction. This approach provided a broad substrate scope of α‐tertiary amine scaffolds from a plethora of C3‐substituted quinolinium and sulfonyl azides. The post‐synthetic modifications have further diversified the α‐tertiary amine core into interesting scaffolds. Preliminary mechanistic studies suggested the involvement of aziridine ring formation for the amine migration to the C‐3 position of quinoline to generate the α‐tertiary amine core.

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Antimalarial drugs

Cited by 2 publications

References 213 publications

Stage -Specific Antimalarial Activity of Alkaloidal Fractions of the Avicennia africana P. Beauv. (Avicenniaceae) Leaf Extract

Stage -Specific Antimalarial Activity of Alkaloidal Fractions of the Avicennia africana P. Beauv. (Avicenniaceae) Leaf Extract

Dearomative Functionalization of Activated Quinolines: Transfer Hydrogenation/Cycloaddition Cascade to Construct α‐Tertiary Amines

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