Hydrazinated geraniol derivatives as potential broad-spectrum antiprotozoal agents.

Autor: Jooste J; Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa., Legoabe LJ; Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa., Ilbeigi K; Laboratory of Microbiology, Parasitology and Hygiene (LMPH), Infla-Med Centre of Excellence, University of Antwerp, Antwerp, Belgium., Caljon G; Laboratory of Microbiology, Parasitology and Hygiene (LMPH), Infla-Med Centre of Excellence, University of Antwerp, Antwerp, Belgium., Beteck RM; Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa.
Jazyk: angličtina
Zdroj: Archiv der Pharmazie [Arch Pharm (Weinheim)] 2024 Oct; Vol. 357 (10), pp. e2400430. Date of Electronic Publication: 2024 Jul 09.
DOI: 10.1002/ardp.202400430
Abstrakt: 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 µM. 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 µM, 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 µM, respectively. Compound 6, with an IC 50 value of 11.73 µM, and compound 14, with an IC 50 value of 8.14 µM, demonstrated some modest antileishmanial activity.
(© 2024 The Author(s). Archiv der Pharmazie published by Wiley‐VCH GmbH on behalf of Deutsche Pharmazeutische Gesellschaft.)
Databáze: MEDLINE