Serine hydrolases are susceptible to potent reversible inhibition by boronic acids. Large collections of chemically diverse boronic acid fragments are commercially available because of their utility in coupling chemistry. We repurposed the approximately 650 boronic acid reagents in our collection as a directed fragment library targeting serine hydrolases and related enzymes. Highly efficient hi...

A series of tetrasubstituted aromatics has been synthesized, many of which are based on elaborated N-methyliminodiacetic acid (MIDA)-boronates. A sequence employing nitration, bromination, stepwise Suzuki-Miyaura (SM) coupling with a boronic acid, then base-mediated unmasking of the boronic acid from the MIDA-boronate and a second SM-coupling has led to our desired, mainly 1,2,4,5-substituted t...

background: ampc type β-lactamases are commonly isolated from extended-spectrum cephalosporin-resistant gram-negative bacteria. also, resistance appeared in bacterial species not naturally producing ampc enzymes. therefore, a standard test for the detection of the plasmid-mediated ampc enzyme and new breakpoints for extended spectrum cephalosporins are urgently necessary. objectives: to detect ...

Class A carbapenemases are a major threat to the potency of carbapenem antibiotics. A widespread carbapenemase, KPC-2, is not easily inhibited by β-lactamase inhibitors (i.e., clavulanic acid, sulbactam, and tazobactam). To explore different mechanisms of inhibition of KPC-2, we determined the crystal structures of KPC-2 with two β-lactamase inhibitors that follow different inactivation pathway...

We report a new water-soluble fluorescent probe sensitive to aqueous fluoride. The probe shows spectral shifts and intensity changes in the presence of fluoride, in a wavelength ratiometric and colorimetric manner, enabling the detection of fluoride concentrations at visible wavelengths, in the concentration range ≈1–300 mM. The probes response is based on the ability of the boronic acid group ...

b ackground : one of the main mechanisms of resistance to carbapenems is potential of klebsiella pneumoniae to produce k . pneumoniae carbapenemase (kpc). kpc is an important type of carbapenemase, which can hydrolyze carbapenems and other beta-lactam antibiotics. modified hodge test (mht) and  use  of  boronic  acid  as  a  kpc  inhibitor  are  two  types  of  phenotypic methods, which are use...

Phenylboronic acid esters are formed by the three common 2-deoxy aldoses: 2-deoxy-d-erythro-pentose ('2-deoxy-d-ribose'), 2-deoxy-d-lyxo-hexose ('2-deoxy-d-galactose'), and 2-deoxy-d-arabino-hexose ('2-deoxy-d-glucose'). The major species that was formed from equimolar quantities of boronic acid and the aldose, was the 3,4-monoester of the pentopyranose in a skew-boat conformation, and the 4,6-...

Bacteria express beta-lactamases to counteract the beneficial action of antibiotics. Benzo[b]-thiophene-2-boronic acid (BZB) derivatives are β-lactamase inhibitors and, as such, promising compounds to be associated with β-lactam antibacterial therapies. The uncharged form of BZB, in particular, is suggested to diffuse through the outer membrane of gram negative bacteria. In this study, through ...

We are developing photonic crystal glucose sensing materials to continuously monitor relatively high glucose concentrations, such as found in blood. We modified our synthetic fabrication methodologies in order to increase the glucose concentration range and to increase the reproducibility of our PCCA fabrication. We have also advanced our understanding of the sensing response by developing a me...

Three organoboron functionalized polyoxometalates have been synthesized using Schiff base chemistry including a boronic acid, its methyl ester and its trimethylene glycol ester. The compounds have been characterized in the solid state by single crystal diffraction (XRD), FT-IR and elemental analysis and in solution using 1H NMR spectroscopy.