Activity of Carbazole, Aminoguanidine and Diamine Anti-infectives against Toxoplasma gondii

bioRxiv (Cold Spring Harbor Laboratory), Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 16, 2025

We report the observation that carbazole anti-infectives developed as antibacterial and antifungal drug leads have activity against tachyzoite-stage growth of Apicomplexan parasite Toxoplasma gondii with IC 50 values low 2 μM. show a phenylthiazole aminoguanidine well inhibits an value 2.1 also tested series 18 analogs diamine SQ109, tuberculosis candidate which likewise has both activity, finding 2.3 all compounds for their in collapsing ΔpH component promotive force, results indicating acted, at least part, protonophore uncouplers. Finally, we investigated correlation between yeast Saccharomyces cerevisiae bacterium Mycobacterium smegmatis , significant correlations collapse proton motive force anti- fungal/antibacterial activity.

Language: Английский

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In vitro and in vivo activity of 1,2,3,4,6-O-pentagalloyl-glucose against Candida albicans

Antimicrobial Agents and Chemotherapy, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 24, 2025

ABSTRACT Invasive fungal infections have become an increasingly serious threat to global human health, underscoring the urgent need for development of new antifungal drugs. In this study, we found a natural polyphenolic compound 1,2,3,4,6-O-pentagalloyl-glucose (PGG), which is present in various plants and herbs. PGG showed broad-spectrum activities, enhancing efficacy fluconazole. Furthermore, could protect mice against gastrointestinal systemic infection with Candida albicans . Our mechanistic studies revealed that exerts its effects partially by binding CaEno1 protein inhibit activity. As crucial therapeutic target, Eno1 has been reported be closely associated cancer, hypertension, infectious diseases. findings indicated PGG, inhibitor, potential candidate further development.

Language: Английский

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Chemoselective Double Allylic Substitutions with Carbon Nucleophiles: Access to Tetrahydroindoles and Tetrahydrocarbazoles

The Journal of Organic Chemistry, Journal Year: 2025, Volume and Issue: unknown

Published: April 22, 2025

A chemoselective double allylic substitution involving two different carbon nucleophiles is described. The reaction relies on a dual catalytic approach, with Lewis acid promoting the first and Pd second step. Starting from simple diols, diversity of polycyclic structures can be obtained, including tetrahydroindole, tetrahydrocarbazole, tetrahydronaphthalene.

Language: Английский

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Synthesis and Characterization of Novel 1,2,4-Triazole-3-thione Schiff bases compounds Containing Tetrahydrocarbazole Moiety

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: 1322, P. 140616 - 140616

Published: Nov. 5, 2024

Language: Английский

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