N-arylsulfonyl hydrazones as inhibitors of IMP-1 metallo-beta-lactamase.
Members of a family of N-arylsulfonyl hydrazones have been identified as novel inhibitors of IMP-1, a metallo-beta-lactamase of increasing prevalence. Structure-activity relationship studies have indicated a requirement for bulky aromatic substituents on each side of the sulfonyl hydrazone backbone for these compounds to serve as efficient inhibitors of IMP-1. Molecular modeling has provided insight into the structural basis for the anti-metallo-beta-lactamase activity exhibited by this class of compounds.
Department of Chemistry, University of Waterloo, 200 University Avenue W., Waterloo, Ontario N2L 3G1, Canada.
Stefan
S
Siemann
Darryl P
DP
Evanoff
Laura
L
Marrone
Anthony J
AJ
Clarke
Thammaiah
T
Viswanatha
Gary I
GI
Dmitrienko
D001409:Bacillus cereus / Q000187:drug effects / Q000201:enzymology; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006835:Hydrazones / Q000138:chemical synthesis* / Q000494:pharmacology*; D007700:Kinetics; D008958:Models, Molecular; D020133:Reverse Transcriptase Polymerase Chain Reaction; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology*; D065093:beta-Lactamase Inhibitors; D001618:beta-Lactamases
D004791:Enzyme Inhibitors; D006835:Hydrazones; D013449:Sulfonamides; D065093:beta-Lactamase Inhibitors; C409201:beta-lactamase IMP-1; D001618:beta-Lactamases