background one of the major clinical problems regarding pseudomonas aeruginosa is attributed to metallo-beta-lactamases (mbl). this group of enzymes is a subset of beta lactamases which belong to group b of ambler classification and cause hydrolysis of carbapenems. based on epidemiological studies conducted worldwide, it is proved that prevalence of genes coding mbls in p. aeruginosa species ar...

Various inhibitors of metallo-beta-lactamases have been reported; however, none are effective for all subgroups. Those that have been found to inhibit the enzymes of subclass B2 (catalytically active with one zinc) either contain a thiol (and show less inhibition towards this subgroup than towards the dizinc members of B1 and B3) or are inactivators behaving as substrates for the dizinc family ...

The C3-symmetric chiral propylated host-type ligands (±)-tris(isonicotinoyl)-tris(propyl)-cyclotricatechylene (L1) and (±)-tris(4-pyridyl-4-benzoxy)-tris(propyl)-cyclotricatechylene (L2) self-assemble with Pd(II) into [Pd6L8](12+) metallo-cages that resemble a stella octangula. The self-assembly of the [Pd6(L1)8](12+) cage is solvent-dependent; broad NMR resonances and a disordered crystal stru...

Carbapenems, 'last-resort' β-lactam antibiotics, are inactivated by zinc-dependent metallo-β-lactamases (MBLs). The host innate immune response withholds nutrient metal ions from microbial pathogens by releasing metal-chelating proteins such as calprotectin. We show that metal sequestration is detrimental for the accumulation of MBLs in the bacterial periplasm, because those enzymes are readily...

Coordination-driven self-assembly has emerged as a powerful bottom-up approach to construct various supramolecular architectures with increasing complexity and functionality. Tetraphenylethylene (TPE) has been incorporated into metallo-supramolecules to build luminescent materials based on aggregation-induced emission. We herein report three generations of ligands with full conjugation of TPE w...

Metallo-β-lactamases (MBLs) are a growing threat to the use of almost all clinically used β-lactam antibiotics. The identification of broad-spectrum MBL inhibitors is hampered by the lack of a suitable screening platform, consisting of appropriate substrates and a set of clinically relevant MBLs. We report procedures for the preparation of a set of clinically relevant metallo-β-lactamases (i.e....

A synthetic method to prepare tricyclic bridged heptenones and hexenones from gold(I)-catalyzed double cycloisomerization of 1,11-dien-3,9-diyne benzoates is described. A divergence in product selectivity was achieved by fine-tuning the steric nature of the ligand of the Au(I) catalyst. In the presence of [MeCNAu(JohnPhos)](+)SbF6(-) (JohnPhos = (1,1'-biphenyl-2-yl)-di-tert-butylphosphine) as t...

In light of the biomedical significance of metallo-β-lactamases (MβLs), ten new mercaptoacetic acid thioester amino acid derivatives were synthesized and characterized. Biological activity assays indicated that all these synthesized compounds are very potent inhibitors of L1, exhibiting an IC50 value range of 0.018-2.9 μM and a K i value range of 0.11-0.95 μM using cefazolin as substrate. Parti...

Bbstract Recent developments involving polymer-supported metal complexes as catalysts in oxidation reactions, using dioxygen, hydrogen peroxide, alkyl hydroperoxides, hypochlorite anion and iodosobenzene as oxidants are reviewed. binding of dioxygen, and in catalysis, along with the structurally closely related metallo-phthalocyanines, oxidative polymerization catalysed by polymer-supported cop...

Metallo β-lactamases is the name given to certain enzymes found in gram negative bacteria belonging to Enter-obacteriaceae which confers resistance to all β-lactam antibiotics including carbapenems except monobactams. They belong to Ambler molecular class B and Bush-Jacoby-Medeiros Group 3.1,2 Resistance to carbapenems due to production of metallo β-lactamases in Gram Negative organisms is an i...