Quinazolinone fungal efflux pump inhibitors. Part 2: In vitro structure-activity relationships of (N-methyl-piperazinyl)-containing derivatives.
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.
Watkins
William J
WJ
Essential Therapeutics, Inc., 850 Maude Ave., Mountain View, CA 94043, USA. w.watkins@gilead.com
Lemoine
Rémy C
RC
Chong
Lee
L
Cho
Aesop
A
Renau
Thomas E
TE
Kuo
Bonnie
B
Wong
Vickie
V
Ludwikow
Maria
M
Garizi
Negar
N
Iqbal
Nadeem
N
Barnard
John
J
Jankowska
Renata
R
Singh
Rajeshwar
R
Madsen
Deidre
D
Lolans
Karen
K
Lomovskaya
Olga
O
Oza
Uma
U
Dudley
Michael N
MN
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
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