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...

Università della Svizzera italiana

How computational chemistry and drug delivery techniques can support the development of new anticancer drugs

Garofalo, Mariangela ; Grazioso, Giovanni ; Cavalli, Andrea ; Sgrignani, Jacopo

In: Molecules, 2020, vol. 25, no. 7, p. 22 p

The early and late development of new anticancer drugs, small molecules or peptides can be slowed down by some issues such as poor selectivity for the target or poor ADME properties. Computer-aided drug design (CADD) and target drug delivery (TDD) techniques, although apparently far from each other, are two research fields that can give a significant contribution to overcome these problems....