title: Quinazolinone fungal efflux pump inhibitors. Part 2: In vitro structure-activity relationships of (N-methyl-piperazinyl)-containing derivatives.
abstract: Structure-activity relationships of a novel series of fungal efflux pump inhibitors with respect to potentiation of the activity of fluconazole against strains of Candida albicans and Candida glabrata over-expressing ABC-type efflux pumps are systematically explored.
authors.affiliation: Essential Therapeutics, Inc., 850 Maude Ave., Mountain View, CA 94043, USA. w.watkins@gilead.com
authors.forename: William J
authors.initials: WJ
authors.lastname: Watkins
authors.forename: Rémy C
authors.initials: RC
authors.lastname: Lemoine
authors.forename: Lee
authors.initials: L
authors.lastname: Chong
authors.forename: Aesop
authors.initials: A
authors.lastname: Cho
authors.forename: Thomas E
authors.initials: TE
authors.lastname: Renau
authors.forename: Bonnie
authors.initials: B
authors.lastname: Kuo
authors.forename: Vickie
authors.initials: V
authors.lastname: Wong
authors.forename: Maria
authors.initials: M
authors.lastname: Ludwikow
authors.forename: Negar
authors.initials: N
authors.lastname: Garizi
authors.forename: Nadeem
authors.initials: N
authors.lastname: Iqbal
authors.forename: John
authors.initials: J
authors.lastname: Barnard
authors.forename: Renata
authors.initials: R
authors.lastname: Jankowska
authors.forename: Rajeshwar
authors.initials: R
authors.lastname: Singh
authors.forename: Deidre
authors.initials: D
authors.lastname: Madsen
authors.forename: Karen
authors.initials: K
authors.lastname: Lolans
authors.forename: Olga
authors.initials: O
authors.lastname: Lomovskaya
authors.forename: Uma
authors.initials: U
authors.lastname: Oza
authors.forename: Michael N
authors.initials: MN
authors.lastname: Dudley
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002175:Candida / Q000187:drug effects* / Q000201:enzymology; D002176:Candida albicans / Q000187:drug effects / Q000201:enzymology; D041221:Candida glabrata / Q000187:drug effects / Q000201:enzymology; D025141:Drug Resistance, Fungal; D004357:Drug Synergism; D015725:Fluconazole / Q000737:chemistry / Q000494:pharmacology; D005656:Fungal Proteins / Q000037:antagonists & inhibitors; D006801:Humans; D049990:Membrane Transport Modulators; D026901:Membrane Transport Proteins / Q000037:antagonists & inhibitors*; D008826:Microbial Sensitivity Tests; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000935:Antifungal Agents; C094693:CDR1 protein, Candida albicans; D005656:Fungal Proteins; D049990:Membrane Transport Modulators; D026901:Membrane Transport Proteins; D010879:Piperazines; D011799:Quinazolines; D015725:Fluconazole