Author/Authors :
Rémy C. Lemoine، نويسنده , , Tomasz W. Glinka، نويسنده , , William J. Watkins، نويسنده , , Aesop Cho، نويسنده , , Jessie Yang، نويسنده , , Nadeem Iqbal، نويسنده , , Rajeshwar Singh، نويسنده , , Deidre Madsen، نويسنده , , Karen Lolans، نويسنده , , Olga Lomovskaya، نويسنده , , Uma Oza، نويسنده , , Michael N. Dudley، نويسنده ,
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.