Imazalil exhibits a broad spectrum of bioactivities and therapeutic potential. It shows significant antifungal activity against various fungi, including Aspergillus fumigatus, Drechslera sorokiniana, and Fusarium culmorum, with MIC values ranging from 0.1 to 5.0 μg/mL. Additionally, it is effective against Colletotrichum capsici, with an ED50 of less than 5.0 μgAi/mL. The compound demonstrates antiviral properties, including moderate inhibition of SARS-CoV-2 in Vero E6 cells and HRCE cells, and has an IC50 value greater than 20,000 nM for SARS-CoV-2 induced cytotoxicity in VERO-6 cells.
Imazalil exhibits diverse bioactivities, including inhibition of mitochondrial division, rescue of yeast growth from Plasmodium Falciparum HSP40-mediated toxicity, and antagonism of thyroid hormone receptor beta signaling. It inhibits the delayed death of malarial parasite plastid, antagonizes farnesoid X receptor signaling, and shows activity as an agonist for peroxisome proliferator-activated receptor gamma signaling and vitamin D receptor signaling. The compound also acts as an inverse agonist for GLP-1 receptor and activates both rat and human pregnane X receptor signaling pathways. It inhibits survival of Plasmodium falciparum in red blood cells, human tyrosyl-DNA phosphodiesterase 1, TDP-43, and alpha-syn.
Moreover, Imazalil inhibits IDO1 enzyme activity with an IC50 value of 23,000 nM and demonstrates cytotoxicity against mouse P815B cells with an LD50 value greater than 25.0 μM. In the enzymatic assay, it shows -0.06% inhibition of human HDAC6 enzyme using a commercial peptide substrate and -8.66% inhibition using a custom peptide substrate.
While the compound exhibited beta-blocking activity in stepwise linear discriminate analysis, it was inactive in this specific assay with an activity value of -3.17. Overall, the diverse bioactivities of Imazalil suggest its potential therapeutic applications in treating fungal infections, malaria, viral infections, and metabolic disorders..
Note: Summary generated by AI. Data source: ChEMBL 