- Design and structure-activity relationships anticandidosic of diazaheteroaryl functionalized by Micha?l acceptors
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Benzimidazole and imidazopyridine heterocycles associated with Micha?l acceptors have shown strong anticandidosic potential in our previous work. After a decade of research, we have designed, synthesized and evaluated the anticandidosic activities of seve
- Aboudramane, Kone,Doumade, Zon,Drissa, Sissouma,Jean-Paul, N'Guessan D.,Mahama, Ouattara,Mamidou, Koné Witabouna,Songuigama, Coulibaly
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p. 117 - 133
(2022/02/14)
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- Imidazopyridinyl-arylpropenone compounds as potential new anti-infective agents
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This paper describes the design by juxtaposition of anti-infectious moieties, a series of hybrid imidazopyridinyl-arylpropenone compounds. These compounds (5a-y) were synthesized by a crotonization reaction of 1-(2-methylimidazo[1,2-a]pyridin-3-yl)ethanone (3) with benzaldehyde derivatives (4). Spectral determination of structure of those compounds was performed by NMR and ESI mass spectroscopy. From the screening of antiparasitic and antimicrobial activities, the compound 5q (IC50 Combining double low line 1.52 μM) was identified for possible development against a chloroquine-resistant strain of Plasmodium falciparum. The compounds 5n, 5s and 5w showed a veterinary interest due to their nematicidal activities (LC100) against Haemonchus contortus from 7.1 to 1.5 nM. Against candidiasis, three other compounds (5e, 5g, 5v) inhibited drug-resistant strains of Candida albicans (MIQ Combining double low line 1.25 to 0.31 μg). This study showed that the arylpropenone functional group vectorised by imidazopyridine could be considered as a new pharmacophore with potential anti-infectious activities.
- Ouattara, Mahama,Sissouma, Drissa,Koné, Mamidou W.,Yavo, William
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p. 850 - 856
(2016/07/06)
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