Antifungal agent 151 

Antifungal agent 151 is a Prp8 intein inhibitor that inhibits the self-splicing process of the Prp8 intein, preventing maturation of the Prp8 protein. Antifungal agent 151 exerts in vitro antifungal activity against Cryptococcus neoformans and Cryptococcus gattii. Antifungal agent 151 can be used for the research of cryptococcus pneumonia^[1].

Antifungal agent 151 (compound B5) (1-64 μg/mL; 48 h) potently inhibits the growth of C. neoformans H99, C. gattii R265, fluconazole-resistant C. neoformans (strain 313), and clinical isolates of C. neoformans with MIC values ranging from 0.5 to 2 μg/mL^[1].
Antifungal agent 151 (compound B5) (8.0 μg/mL; until fungal elimination) exhibits rapid, concentration-dependent fungicidal activity against C. neoformans H99, eliminating the fungus within two hours^[1].
Antifungal agent 151 (compound B5) (2.0 μg/mL; 2 h) induces transcriptomic remodeling and inhibits proper intron splicing in C. neoformans H99, leading to oxidative stress, DNA damage responses, and altered metabolic gene expression^[1].
Antifungal agent 151 (compound B5) binds to the Prp8 intein active site via hydrogen bonds and a favorable distance for covalent interaction with Cys1^[1].
Antifungal agent 151 (compound B5) has IC₅₀ values of 14.99 μg/mL against LO2 cells and 10.31 μg/mL against A549 cells. Antifungal agent 151shows a lower MIC value against C. neoformans, conferring a higher therapeutic index than 6G-318S^[1].
Antifungal agent 151 (compound B5) (64 μg/mL) shows good blood compatibility with a 3.2% hemolysis rate at 64 μg/mL^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Antifungal agent 151 (compound B5) (10 mg/kg; i.p.; daily; 7 days) effectively reduces fungal burden and pathological damage in a mouse model of C. neoformans pneumonia with favorable biosafety^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

377.41

C₁₆H₁₂FN₃O₃S₂

3097563-43-1

FC1=CC=C(NC(C2=C(S(C3=CC=C(C)C=C3)(=O)=O)SN=N2)=O)C=C1

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• [1]. Tao Y, et al. Design, synthesis, and antifungal evaluation of Prp8 Intein-targeting small molecule inhibitors against Cryptococcus neoformans. Bioorg Chem. 2026;170:109490.  [Content Brief]