Diversity-oriented synthesis and antibiofilm evaluation of furan-2-carboxamides.

A diversity-oriented collection of furan-2-carboxamides with antibiofilm activity against P. aeruginosa is reported. The design involved the bioisosteric replacement of the labile furanone ring by a furan-2-carboxamide moiety to explore its influence on biological activity.

Identification of Potential Inhibitors of Amidases: An Integrated In Silico and Experimental Study.

Virtual screening is a crucial tool in early stage drug discovery for identifying potential hit candidates. Here, we present an integrated approach that combines theoretical and experimental techniques to identify, for the first time, inhibitors of amidases (Ami1-Ami4) from . Through computational methods, we proposed a set of potential inhibitors, which were subsequently evaluated experimentally using differential scanning fluorimetry.

N-acyl-4-arylaminopiperidines: Design and synthesis of a potential antimicrobial scaffold.

We report a concise synthesis of N-acylated piperidines through a Knoevenagel-Doebner condensation/amide construction/ amination sequence. The design of the piperidines considered the pharmacophoric features found in previously reported inhibitors of FabI, an enzyme implicated in bacterial fatty acid biosynthesis. After the microbiological evaluation at 50 μM, the analogs displayed moderate activity against some pathogens from the ESKAPE group, reaching up to 42 % of growth inhibition for MRSA, 54 % for K.

Discovery of dual-action phenolic 4-arylidene-isoquinolinones with antioxidant and α-glucosidase inhibition activities.

A multicomponent-derived synthesis of arylidene isoquinolinones decorated with phenolic moieties is described. The series demonstrated good DPPH trapping and, in the case of sinapic acid-containing analogs, excellent activity against lipoperoxidation; EPR also demonstrated that one derivative scavenged hydroxyl radicals. In addition, some compounds showed excellent inhibition of α-glucosidase activity and, according to both Lineweaver-Burk plots and molecular docking, they act as non-competitive or mixed inhibitors.

Synthesis, antibiofilm activity and molecular docking of N-acylhomoserine lactones containing cinammic moieties.

We prepared a series of cinnamoyl-containing furanones by an affordable and short synthesis. The nineteen compounds hold a variety of substituents including electron-donating, electron-withdrawing, bulky and meta-substituted phenyls, as well as heterocyclic rings. Compounds showed antibiofilm activity in S.