Antifungal agent 22 (compound D16) 是一种潜在的口服有效的抗真菌药物，其IC50值为 0.5 μg/mL。Antifungal agent 22 能穿透血脑屏障，通过破坏真菌细胞膜的完整性杀死C. neoformansH99 细胞。Antifungal agent 22 具有选择性抗隐球菌活性，代谢稳定性好，细胞毒性低。

Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with an IC 50 of 0.5 μg/mL. Antifungal agent 22 can penetrate the blood-brain barrier and kill the C. neoformans H99 cells by destroying the integrity of fungal cell membranes. Antifungal agent 22 shows selective anti- Cryptococcus activity with good metabolic stability and low cytotoxicity [1].

Antifungal agent 22 (compound D16) (0-1 μg/mL, 24 h) inhibits ergosterol biosynthesis, which results in stress-induced upregulation of ERG genes in C. neoformans H99 [1]. Antifungal agent 22 (0-8 μg/mL) effectively inhibits the growth of C. neoformans H99 (0-72 h), inhibits the formation of C. neoformans H99 biofilms in a concentration-dependent manner (24 h) [1]. Antifungal agent 22 (0-8 μg/mL, 48-72 h) shows selective anti- Cryptococcus activity, has a fungistatic effect [1]. Antifungal agent 22 (0-100 μM, 48 h) shows low cytotoxicity against a human HUVEC cell line with an IC 50 of 20.18 μM [1]. Cell Proliferation Assay Cell Line: C. neoformans H99 cells [1] Concentration: 0, 1, 2, 4, 8 μg/mL Incubation Time: 0, 4, 8, 12, 24, 48, and 72 h Result: Almost completely inhibited the growth of C. neoformans H99 at 8 μg/mL, remained at nearly 100% inhibition rate after 72 h, had minimum fungicidal concentrations of 8 μg/mL. Cell Viability Assay Cell Line: Fungal cells (RPMI 1640 medium) [1] Concentration: 0, 0.5, 1, 2, 4, 8 μg/mL Incubation Time: 48, 72 h Result: Showed selective anti- Cryptococcus activity, with IC 50 range of 0.06-2 μg/mL and a MIC 50 value (average IC 50 values) of 0.62 μg/mL.

Antifungal agent 22 (D16) (15 mg/kg, Intragastrically, daily for 5 days) shows potent anti- Cryptococcal efficacy [1]. Animal Model: ICR female mice (18-22 g, 4-6 weeks, tail vein injected with C. neoformans H99 cells) [1] Dosage: 15 mg/kg Administration: Intragastrically, daily for 5 days Result: Showed potent anti- Cryptococcal efficacy, significantly reduced the number of C. neoformans H99 cells in the brain after 5 days, prolong the median survival time (14 days) of the infected mice at a dose of 15 mg/kg.

2640054-39-1

C21H26Cl3NOS

446.86

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years