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Acanthamoeba castellanii
is an opportunistic pathogen with public health implications, largely due to its invasive nature and non-specific symptoms. Our study focuses on the potential of azole compounds, particularly those with triazole scaffolds, as anti-amoebic agents. Out of 10 compounds, compounds
T1
and
T8
exhibited effective anti-
Acanthamoeba
activity with MIC
50
values of 125.37 and 143.92 μg mL
−1
, respectively. Interestingly, compounds
T1
,
T4
,
T5
and
T8
revealed profound anti-excystation activity with MIC
50
at 32.01, 85.53, 19.54 and 80.57 g mL
−1
, respectively, alongside limited cytotoxicity to human cells. The study underscores the potential of
T1
,
T4
,
T5
, and
T8
, thiazole-based compounds, as anti-
Acanthamoeba
agents by both eliminating amoeba viability and preventing excystation,
via
preserving the amoeba in its latent cyst form, exposing them to elimination by the immune system. Notably, compounds
T1
,
T4
,
T5
, and
T8
showed optimal molecular properties, moderate oral bioavailability, and stable complex formation with
Acanthamoeba
CYP51. They also display superior binding interactions. Further research is needed to understand their mechanisms and optimize their efficacy against
Acanthamoeba
infections.
New azole derivatives against
Acanthamoeba castellanii
.
Sprache
–
Identifikatoren
eISSN: 2632-8682
DOI: 10.1039/d4md00029c
Titel-ID: cdi_rsc_primary_d4md00029c
Format
–
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