Hydrazinated geraniol derivatives as potential broad‐spectrum antiprotozoal agents

Author:

Jooste Joelien1,Legoabe Lesetja J.1,Ilbeigi Kayhan2,Caljon Guy2,Beteck Richard M.1

Affiliation:

1. Centre of Excellence for Pharmaceutical Sciences North‐West University Potchefstroom South Africa

2. Laboratory of Microbiology, Parasitology and Hygiene (LMPH), Infla‐Med Centre of Excellence University of Antwerp Antwerp Belgium

Abstract

AbstractGeraniol, 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 IC50 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 IC50 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 IC50 values of 5.14, 6.30 and 4.90 µM, respectively. Compound 6, with an IC50 value of 11.73 µM, and compound 14, with an IC50 value of 8.14 µM, demonstrated some modest antileishmanial activity.

Funder

South African Medical Research Council

Publisher

Wiley

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