Structure-activity relationships of biphenyl tetrazoles as metallo-beta-lactamase inhibitors.
Resistance to carbapenem antibiotics in gram-negative bacteria is due, in part, to expression of a wide spectrum metallo-beta-lactamase, which renders the drug inactive. Biphenyl tetrazoles containing 3-n-butyl-1-phenylpyrazole-5-carboxylates or the corresponding 5-ethyl esters were found to inhibit metallo-beta-lactamases as well as renal dehydropeptidase I to a lesser extent.
Toney
J H
JH
Department of Biochemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA.
Cleary
K A
KA
Hammond
G G
GG
Yuan
X
X
May
W J
WJ
Hutchins
S M
SM
Ashton
W T
WT
Vanderwall
D E
DE
D001441:Bacteroides fragilis / Q000201:enzymology; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013777:Tetrazoles / Q000737:chemistry* / Q000494:pharmacology*; D065093:beta-Lactamase Inhibitors
D004791:Enzyme Inhibitors; D013777:Tetrazoles; D065093:beta-Lactamase Inhibitors