19F-NMR reveals the role of mobile loops in product and inhibitor binding by the São Paolo metallo-β-lactamase

Autor: Martine I. Abboud, Philip Hinchliffe, Jürgen Brem, Robert Macsics, Inga Pfeffer, Anne Makena, Klaus-Daniel Umland, Anna M. Rydzik, Guo-Bo Li, James Spencer, Timothy D. W. Claridge, Christopher J. Schofield

Publikováno v: Abboud, M I, Hinchliffe, P, Brem, J, Macsics, R, Pfeffer, I, Makena, A, Umland, K-D, Rydzik, A M, Li, G-B, Spencer, J, Claridge, T D W & Schofield, C J 2017, ' 19 F-NMR Reveals the Role of Mobile Loops in Product and Inhibitor Binding by the São Paulo Metallo-β-Lactamase ', Angewandte Chemie-International Edition, vol. 56, no. 14, pp. 3862–3866 . https://doi.org/10.1002/anie.201612185

Resistance to beta-lactam antibiotics mediated by metallo-beta-lactamases (MBLs) is a growing problem. We describe the use of protein-observe 19F-NMR (PrOF NMR) to study the dynamics of the São Paulo MBL (SPM-1) from beta-lactam- resistant Pseudomon

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Oxidative Chlorination of Activated Methylene Compounds with Sodium Chloride

Autor: Camilla Mayer, Klaus‐Daniel Umland, Stefan F. Kirsch

Publikováno v: Synlett. 25:813-816

An operationally simple protocol for the direct chlorination of 1,3-dicarbonyls (and related compounds such as α-cyano ­ketones) is described. The procedure relies on mild conditions using IBX–SO3K as the stoichiometric oxidizing agent and the ub

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https://doi.org/10.1055/s-0033-1340793

Sideromimic Modification of Lactivicin Dramatically Increases Potency against Extensively Drug-Resistant Stenotrophomonas maltophilia Clinical Isolates

Autor: Philip Hinchliffe, James Spencer, Karina Calvopiña, Jürgen Brem, Matthew B. Avison, Christopher J. Schofield, Anna M. Rydzik, Klaus-Daniel Umland

Publikováno v: Calvopiña, K, Umland, K-D, Rydzik, A M, Hinchliffe, P, Brem, J, Spencer, J, Schofield, C J & Avison, M B 2016, ' Sideromimic Modification of Lactivicin Dramatically Increases Potency against Extensively Drug-Resistant Stenotrophomonas maltophilia Clinical Isolates ', Antimicrobial Agents and Chemotherapy, vol. 60, no. 7, pp. 4170-4175 . https://doi.org/10.1128/AAC.00371-16

Acetamido derivatives of the naturally antibacterial non-β-lactam lactivicin (LTV) have improved activity against their penicillin binding protein targets and reduced hydrolysis by β-lactamases, but penetration into Gram-negative bacteria is still

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Elektrophile Cyclisierung von 1,5-Eninen

Autor: Klaus‐Daniel Umland, Stefan F. Kirsch, Benedikt Crone

Publikováno v: Angewandte Chemie. 122:4765-4768

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https://doi.org/10.1002/ange.201001113

In vitro and in vivo activity of ML302F: a thioenolate inhibitor of VIM-subfamily metallo β-lactamases

Autor: Jürgen Brem, Lynette M. Phee, David W. Wareham, Muhd Haziq F Abdul Momin, Jonathan W. Betts, Klaus-Daniel Umland, Christopher J. Schofield

Publikováno v: MedChemComm. 7(1)

The thioenol ML302F was recently identified as an inhibitor of class B metallo-β-lactamases (MBLs). We assessed the activity of ML302F when combined with meropenem (MEM) against 31 carbapenem resistant Gram-negative clinical isolates. Minimum inhibi

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