Chemical communications (Cambridge, England), 2018-12, Vol.54 (96), p.13535-13538
2018
Volltextzugriff (PDF)
Details
- Autor(en) / Beteiligte
- Titel
- Novel non-peptidic small molecule inhibitors of secreted aspartic protease 2 (SAP2) for the treatment of resistant fungal infections
- Ist Teil von
- Chemical communications (Cambridge, England), 2018-12, Vol.54 (96), p.13535-13538
- Ort / Verlag
- England: Royal Society of Chemistry
- Erscheinungsjahr
- 2018
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- Targeting secreted aspartic protease 2 (SAP2), a kind of virulence factor, represents a new strategy for antifungal drug discovery. In this report, the first-generation of small molecule SAP2 inhibitors was rationally designed and optimized using a structure-based approach. In particular, inhibitor 23h was highly potent and selective and showed good antifungal potency for the treatment of resistant Candida albicans infections.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 1359-7345eISSN: 1364-548XDOI: 10.1039/c8cc07810fTitel-ID: cdi_proquest_miscellaneous_2133827663
- Format
- –
- Schlagworte
- Animals, Antifungal Agents - chemical synthesis, Antifungal Agents - chemistry, Antifungal Agents - therapeutic use, Antifungal Agents - toxicity, Aspartic Acid Proteases - antagonists & inhibitors, Aspartic Acid Proteases - chemistry, Caenorhabditis elegans, Candida albicans - drug effects, Candidiasis - drug therapy, Female, Fungal Proteins - antagonists & inhibitors, Fungal Proteins - chemistry, Fungicides, Humans, Mice, Inbred ICR, Molecular Docking Simulation, Protease, Protease inhibitors, Protease Inhibitors - chemical synthesis, Protease Inhibitors - chemistry, Protease Inhibitors - therapeutic use, Protease Inhibitors - toxicity, Structure-Activity Relationship, Thiazolidines - chemical synthesis, Thiazolidines - chemistry, Thiazolidines - therapeutic use, Thiazolidines - toxicity, Virulence, Virulence Factors - antagonists & inhibitors, Virulence Factors - chemistry