Five series of heterocyclic tripartite 2,6-difluorobenzamides, namely 1,2,3-triazoles, 1,2,4- and 1,3,4-oxadiazoles, analogs of reported model anti-staphylococcal compounds, were prepared. The purpose was to investigate the influence of the nature of the heterocyclic central scaffold on the biological activity against three strains of including two drug-resistant ones. Among the 15 compounds of the new collection, a 3-(4--butylphenyl)-1,2,4-oxadiazole linked via a methylene group with a 2,6-difluorobenzamide moiety () exhibited a minimal inhibitory concentration between 0.
View Article and Find Full Text PDFThe benzo[]thiophene nucleus and the acylhydrazone functional group were combined to prepare three new series of compounds for screening against . The reaction of substituted benzo[]thiophene-2-carboxylic hydrazide and various aromatic or heteroaromatic aldehydes led to a collection of 26 final products with extensive structural diversification on the aromatic ring and on position 6 of the benzo[]thiophene nucleus. The screening lead to the identification of eight hits, including ()-6-chloro-'-(pyridin-2-ylmethylene)benzo[]thiophene-2-carbohydrazide (), a non-cytotoxic derivative showing a minimal inhibitory concentration of 4 µg/mL on three strains, among which were a reference classical strain and two clinically isolated strains resistant to methicillin and daptomycin, respectively.
View Article and Find Full Text PDFPurpose: To determine the value of IL-10 measurement in aqueous humor (AH) for screening in primary intraocular lymphoma (PIOL).
Methods: One hundred consecutive diagnostic or therapeutic vitrectomies were performed in patients with uveitis. During surgery, 100 microL of both AH and pure vitreous was taken.