Hydrazinated geraniol derivatives as potentialbroad‐spectrum antiprotozoal agents

Abstract

Geraniol, a primary component of several essential oils, has been associated withbroad‐spectrum antiprotozoal activities, although moderate to weak. This studyprimarily concentrated on the synthesis of hydrazinated geraniol derivatives aspotential antiprotozoal agents. The synthesised compounds were tested in vitroagainst different parasitic protozoans of clinical relevance, including Trypanosomabrucei brucei, Trypanosoma brucei rhodesiense, Trypanosoma cruzi and Leishmaniainfantum. Compounds 6, 8, 13, 14 and 15 demonstrated low micromolar activityagainst the different parasites. Compounds 8, 13, 14 and 15 had the highest efficacyagainst Trypanosoma brucei rhodesiense, as indicated by their respective IC 50 valuesof 0.74, 0.56, 1.26 and 1.00 μM. Compounds 6, 14 and 15 displayed the best activityagainst 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 intracellularTrypanosoma 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 valueof 8.14 μM, demonstrated some modest antileishmanial activity