AOA-2 Derivatives as Outer Membrane Protein A Inhibitors for Treatment of Gram-Negative Bacilli Infections.

Previously, we identified that a cyclic hexapeptide AOA-2 inhibited the interaction of Gram-negative bacilli (GNB) like , , and to host cells thereby preventing the development of infection and in a murine sepsis peritoneal model. In this work, we aimed to evaluate a library of AOA-2 derivatives in order to improve the effect of AOA-2 against GNB infections. Ten AOA-2 derivatives were synthetized for the assays.

A fluorous sodium l-prolinate derivative as low molecular weight gelator for perfluorocarbons.

We report the first study dealing with the self-assembly of an α-amino acid derivative in perfluorocarbons. Rheology, microscopy, and spectroscopy studies reveal that the fluorous sodium l-prolinate derivative 1 self-assembles in perfluorocarbons to form a three-dimensional network of left-handed nano-helices resulting in solvent gelation. Singlet oxygen lifetime measured in a gel of perfluorodecalin is about 1000 times longer than in pure water.

Synergistic activity of an OmpA inhibitor and colistin against colistin-resistant Acinetobacter baumannii: mechanistic analysis and in vivo efficacy.

Objectives: Preventing bacterial contact with host cells can provide an additional approach to tackling MDR Acinetobacter baumannii. Recently, we identified AOA-2 as a potential blocker of A. baumannii outer membrane protein A without presenting bactericidal activity.

Combating virulence of Gram-negative bacilli by OmpA inhibition.

Preventing the adhesion of pathogens to host cells provides an innovative approach to tackling multidrug-resistant bacteria. In this regard, the identification of outer membrane protein A (OmpA) as a key bacterial virulence factor has been a major breakthrough. The use of virtual screening helped us to identify a cyclic hexapeptide AOA-2 that inhibits the adhesion of Acinetobacter baumannii, Pseudomonas aeruginosa and Escherichia coli to host cells and the formation of biofilm, thereby preventing the development of infection in vitro and in a murine sepsis peritoneal model.

Effective ascorbate-free and photolatent click reactions in water using a photoreducible copper(II)-ethylenediamine precatalyst.

The search for copper catalysts able to perform effectively click reactions in water in the absence of sodium ascorbate is an active area of current research with strong potential for applications in bioconjugation. The water-soluble and photoreducible copper(II)-EDA (EDA = ethylenediamine) complex 1, which has two 4-benzoylbenzoates acting as both counterion and photosensitizer, has been synthesized and characterized by different techniques including single crystal X-ray diffraction. Highly efficient photoreduction was demonstrated when solutions of 1 in hydrogen atom donating solvents, such as THF or MeOH, were exposed to UVA radiation (350-400 nm) provided by a low pressure mercury lamp (type TLC = thin-layer chromatography, 365 nm), or by a 23 W fluorescent bulb, or by ambient/sunlight.