Abstract
Further structure-activity relationships of a novel series of fungal efflux pump inhibitors with respect to potentiation of the activity of fluconazole against strains of C. albicans and C. glabrata over-expressing ABC-type efflux pumps are systematically explored. Rat protein binding and pharmacokinetics of selected analogues are reported.
MeSH terms
-
Animals
-
Antifungal Agents / blood
-
Antifungal Agents / chemistry
-
Antifungal Agents / pharmacokinetics
-
Antifungal Agents / pharmacology*
-
Candida albicans / drug effects
-
Hepatocytes / metabolism
-
Male
-
Membrane Transport Proteins / drug effects*
-
Membrane Transport Proteins / metabolism
-
Molecular Structure
-
Piperazine
-
Piperazines / chemistry*
-
Quinazolinones / blood
-
Quinazolinones / pharmacokinetics
-
Quinazolinones / pharmacology*
-
Rats
-
Rats, Sprague-Dawley
-
Serum / chemistry*
-
Structure-Activity Relationship
Substances
-
Antifungal Agents
-
Membrane Transport Proteins
-
Piperazines
-
Quinazolinones
-
Piperazine