Quinazolinone-based fungal efflux pump inhibitors. Part 1: Discovery of an (N-methylpiperazine)-containing derivative with activity in clinically relevant Candida spp.
Bioorg Med Chem Lett
; 14(20): 5127-31, 2004 Oct 18.
Article
in En
| MEDLINE
| ID: mdl-15380213
ABSTRACT
The discovery of a series of quinazolinone-based fungal efflux pump inhibitors by high-throughput screening for potentiation of fluconazole in C. albicans is described. Attempts to improve the aqueous solubility of screening hits led to the discovery of an analog with greatly improved physical properties and activity against clinically-relevant Candida spp.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Membrane Transport Proteins
/
Piperazines
/
Quinazolines
/
Candida
/
Fungal Proteins
/
ATP-Binding Cassette Transporters
/
Membrane Transport Modulators
/
Antifungal Agents
Limits:
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Year:
2004
Document type:
Article