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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
3-Mercapto-1,2,4-triazoles and N-acylated thiosemicarbazides as metallo-β-lactamase inhibitors
Bioorganic and Medicinal Chemistry Letters, Volume 22, No. 1, Year 2012
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Description
The production of β-lactamases is an effective strategy by which pathogenic bacteria can develop resistance against β-lactam antibiotics. While inhibitors of serine-β-lactamases are widely used in combination therapy with β-lactam antibiotics, there are no clinically available inhibitors of metallo-β-lactamases (MBLs), and so there is a need for the development of such inhibitors. This work describes the optimisation of a lead inhibitor previously identified by fragment screening of a compound library. We also report that thiosemicarbazide intermediates in the syntheses of these compounds are also moderately potent inhibitors of the IMP-1 MBL from Pseudomonas aeruginosa. The interactions of these inhibitors with the active site of IMP-1 were examined using in silico methods. © 2011 Elsevier Ltd. All rights reserved.
Authors & Co-Authors
Faridoon,
Australia, Brisbane
The University of Queensland
Pakistan, Peshawar
University of Peshawar
Hussein, Waleed M.
Australia, Brisbane
The University of Queensland
Egypt, Helwan
Faculty of Pharmacy
Vella, Peter
Australia, Brisbane
The University of Queensland
Islam, Nazar Ul
Pakistan, Peshawar
University of Peshawar
Ollis, David L.
Australia, Canberra
The Australian National University
Schenk, Gerhard
Australia, Brisbane
The University of Queensland
Ireland, Maynooth
Maynooth University
McGeary, Ross P.
Australia, Brisbane
The University of Queensland
Statistics
Citations: 70
Authors: 7
Affiliations: 5
Identifiers
Doi:
10.1016/j.bmcl.2011.10.116
ISSN:
0960894X
e-ISSN:
14643405