Antifungal agent 22

Modify Date: 2024-01-23 10:10:57

Antifungal agent 22 Structure
Antifungal agent 22 structure
Common Name Antifungal agent 22
CAS Number 2640054-39-1 Molecular Weight 446.86
Density N/A Boiling Point N/A
Molecular Formula C21H26Cl3NOS Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Antifungal agent 22


Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with an IC50 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].

 Names

Name Antifungal agent 22

 Antifungal agent 22 Biological Activity

Description Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with an IC50 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].
Related Catalog
Target

IC50: 0.5 μg/mL (Fungal)[1].

In Vitro 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 IC50 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 IC50 range of 0.06-2 μg/mL and a MIC50 value (average IC50 values) of 0.62 μg/mL.
In Vivo 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.
References

[1]. Li W, Yun Z, Ji C, et al. Discovery of Novel Sertraline Derivatives as Potent anti-Cryptococcus Agents.J Med Chem. 2022 Mar 6;10.1021/acs.jmedchem.1c01845.

 Chemical & Physical Properties

Molecular Formula C21H26Cl3NOS
Molecular Weight 446.86