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PDBsum entry 5mxr
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References listed in PDB file
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Key reference
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Title
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Sar studies leading to the identification of a novel series of metallo-β-Lactamase inhibitors for the treatment of carbapenem-Resistant enterobacteriaceae infections that display efficacy in an animal infection model.
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Authors
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S.Leiris,
A.Coelho,
J.Castandet,
M.Bayet,
C.Lozano,
J.Bougnon,
J.Bousquet,
M.Everett,
M.Lemonnier,
N.Sprynski,
M.Zalacain,
T.D.Pallin,
M.C.Cramp,
N.Jennings,
G.Raphy,
M.W.Jones,
R.Pattipati,
B.Shankar,
R.Sivasubrahmanyam,
A.K.Soodhagani,
R.R.Juventhala,
N.Pottabathini,
S.Pothukanuri,
M.Benvenuti,
C.Pozzi,
S.Mangani,
F.De luca,
G.Cerboni,
J.D.Docquier,
D.T.Davies.
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Ref.
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ACS Infect Dis, 2019,
5,
131-140.
[DOI no: ]
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PubMed id
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Abstract
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The clinical effectiveness of carbapenem antibiotics such as meropenem is
becoming increasingly compromised by the spread of both metallo-β-lactamase
(MBL) and serine-β-lactamase (SBL) enzymes on mobile genetic elements,
stimulating research to find new β-lactamase inhibitors to be used in
conjunction with carbapenems and other β-lactam antibiotics. Herein, we
describe our initial exploration of a novel chemical series of
metallo-β-lactamase inhibitors, from concept to efficacy, in a survival model
using an advanced tool compound (ANT431) in conjunction with meropenem.
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