CYP51-IN-22 is a potent and broad-spectrum CYP51 inhibitor, and it is the non-deuterated form of CYP51-IN-23-d3, with an MIC80 of 1 μg/mL against Aspergillus fumigatus. It exhibits resistance-modulating activity and bactericidal properties, demonstrating good safety in cells and significant pharmacodynamic activity in mice. CYP51-IN-22 is applicable for research on invasive fungal infections (IFIs).

CYP51-IN-22 (Compound V23) demonstrates broad-spectrum activity against eight fluconazole-resistant fungi with an MIC 80 of 1-16 μg/ml over a period of 48 hours. It exerts bactericidal effects on Candida parapsilosis in a dose-dependent manner (2-8×MIC, 0-24 h), improving with higher concentrations and longer exposure. During the biofilm development phase, CYP51-IN-22 (0-32 ml, 6 h) effectively inhibits biofilm formation in Candida glabrata and Cryptococcus neoformans. Furthermore, this compound can suppress the morphological transition of Candida albicans (2-8 ml, 4 h). Its toxicity is negligible when tested on HUVEC (human umbilical vein endothelial cells) and SH-SY5Y (neuroblastoma cell line) at a concentration of 10 μM over 4 hours.

CYP51-IN-22 (Compound V23), administered intraperitoneally at a dosage of 10 mg/kg following infection by 4 hours, demonstrated exceptional therapeutic efficacy in a mouse model of invasive candidiasis.