1. Quinazolinone fungal efflux pump inhibitors. Part 3: (N-methyl)piperazine variants and pharmacokinetic optimization
- Author
-
Aesop Cho, David C. Griffith, Lee Chong, Nadeem Iqbal, Padmapriya Kumaraswamy, Uma Oza, Michael N. Dudley, Karen Lolans, Maria Ludwikow, David J. Loury, Shuang Bai, Rajeshwar Singh, Andrea Blecken, Ramona Hilgenkamp, William J. Watkins, Olga Lomovskaya, Deidre Madsen, John Barnard, and Negar Garizi
- Subjects
Male ,Serum ,Antifungal Agents ,medicine.drug_class ,Clinical Biochemistry ,Pharmaceutical Science ,Diaphragm pump ,Carboxamide ,Biochemistry ,Piperazines ,Rats, Sprague-Dawley ,Structure-Activity Relationship ,chemistry.chemical_compound ,Pharmacokinetics ,Candida albicans ,Drug Discovery ,medicine ,Animals ,Piperazine ,Molecular Biology ,Quinazolinone ,Quinazolinones ,Molecular Structure ,biology ,Candida glabrata ,Chemistry ,Organic Chemistry ,Membrane Transport Proteins ,biology.organism_classification ,Rats ,Hepatocytes ,Molecular Medicine ,Efflux - 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.
- Published
- 2007