Università della Svizzera italiana

Isonitrile-based multicomponent synthesis of β-amino boronic acids as β-lactamase inhibitors

Bassini, Emanuele ; Gazzotti, Stefano ; Sannio, Filomena ; Lo Presti, Leonardo ; Sgrignani, Jacopo ; Docquier, Jean-Denis ; Grazioso, Giovanni ; Silvani, Alessandra

In: Antibiotics, 2020, vol. 9, no. 5, p. 21 p

The application of various isonitrile-based multicomponent reactions to protected (2-oxoethyl)boronic acid (as the carbonyl component) is described. The Ugi reaction, both in the four components and in the four centers–three components versions, and the van Leusen reaction, proved effective at providing small libraries of MIDA-protected β-aminoboronic acids. The corresponding free...

Université de Fribourg

Crystal structure of the Pseudomonas aeruginosa BEL-1 extended-spectrum β-lactamase and its complexes with moxalactam and imipenem

Pozzi, Cecilia ; Luca, Filomena De ; Benvenuti, Manuela ; Poirel, Laurent ; Nordmann, Patrice ; Rossolini, Gian Maria ; Mangani, Stefano ; Docquier, Jean-Denis

In: Antimicrobial Agents and Chemotherapy, 2016, vol. 60, no. 12, p. 7189–7199

BEL-1 is an acquired class A extended-spectrum β-lactamase (ESBL) found in Pseudomonas aeruginosa clinical isolates from Belgium which is divergent from other ESBLs (maximum identity of 54% with GES-type enzymes). This enzyme is efficiently inhibited by clavulanate, imipenem, and moxalactam. Crystals of BEL-1 were obtained at pH 5.6, and the structure of native BEL-1 was determined from...