Hydrazinated geraniol derivatives as potential broad-spectrum antiprotozoal agents.

Abstract:

Geraniol, a primary component of several essential oils, has been associated with broad-spectrum antiprotozoal activities, although moderate to weak. This study primarily concentrated on the synthesis of hydrazinated geraniol derivatives as potential antiprotozoal agents. The synthesised compounds were tested in vitro against different parasitic protozoans of clinical relevance, including Trypanosoma brucei brucei, Trypanosoma brucei rhodesiense, Trypanosoma cruzi and Leishmania infantum. Compounds 6, 8, 13, 14 and 15 demonstrated low micromolar activity against the different parasites. Compounds 8, 13, 14 and 15 had the highest efficacy against Trypanosoma brucei rhodesiense, as indicated by their respective IC(50) values of 0.74, 0.56, 1.26 and 1.00 microM. Compounds 6, 14 and 15 displayed the best activity against Trypanosoma brucei brucei, with IC(50) values of 1.49, 1.48 and 1.85 microM, respectively. The activity of compounds 6, 14 and 15 also extended to intracellular Trypanosoma cruzi, with IC(50) values of 5.14, 6.30 and 4.90 microM, respectively. Compound 6, with an IC(50) value of 11.73 microM, and compound 14, with an IC(50) value of 8.14 microM, demonstrated some modest antileishmanial activity.

Citation: Arch Pharm (Weinheim). 2024 Oct;357(10):e2400430. doi: 10.1002/ardp.202400430. Epub 2024 Jul 9.

Date Published: 4th Oct 2024

Registered Mode: by PubMed ID

Authors: J. Jooste, L. J. Legoabe, K. Ilbeigi, G. Caljon, R. M. Beteck

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Created: 14th Jul 2026 at 07:53

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