Journal: RSC Medicinal Chemistry

Article Title: Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria † †Electronic supplementary information (ESI) available: Synthesis and characterization data of compounds ( 1 H, 13 C NMR and HRMS). Bacterial strains, media, cell lines and reagents used. Protocols for the determination of the MICs and MBCs against bacteria, synergy of compounds with standard antibiotics, in vitro cytotoxicity analysis of compounds 6 , 11 , 12 and 13 against human colorectal and murine macrophage cells, hemolysis assay, time-kill kinetics analysis, intracellular infection of J774 cells with MRSA and treatment with compounds 6 and 12 . Table of bacterial isolates used in this study. See DOI: 10.1039/c9md00391f

doi: 10.1039/c9md00391f

Figure Lengend Snippet: The minimum inhibitory concentrations (MICs in μg mL –1 ) of compounds 6 , 11 , 12 and 13 against a panel of clinically important Gram-positive bacterial pathogens including Staphylococcus epidermidis , Streptococcus pneumoniae, Enterococcus faecalis , Enterococcus faecium and Listeria monocytogenes

Article Snippet: 24 table ft1 table-wrap mode="anchored" t5 caption a7 Bacterial strains a Compounds/control antibiotics 6 11 12 13 Vancomycin Linezolid Methicillin-sensitive Staphylococcus aureus ATCC 6538 8 1 0.5 0.5 1 0.5 Methicillin-sensitive Staphylococcus aureus NRS 107 4 1 0.25 0.125 1 0.5 MRSA NRS 119 8 1 0.5 0.06 1 >64 MRSA NRS382 (USA100) 8 1 0.5 0.5 2 1 MRSA NRS383 (USA200) 8 2 0.25 1 1 1 MRSA NRS384 (USA300) 4 0.5 0.5 0.5 1 1 MRSA NRS123 (USA400) 4 1 0.5 0.25 1 1 MRSA NRS 385 (USA500) 8 2 2 0.5 2 1 MRSA NRS 386 (USA700) 4 1 0.5 0.125 1 1 MRSA NRS 387 (USA800) 4 2 0.125 0.25 2 1 MRSA NRS 483 (USA1000) 4 1 0.5 0.25 2 1 MRSA NRS 484 (USA1100) 4 0.5 0.5 0.5 2 2 VRSA 10 4 1 0.5 0.25 >64 1 VRSA 12 8 1 0.5 0.125 >64 1 Open in a separate window a See ESI for sources of bacterial strains. caption a8 The minimum inhibitory concentrations (MICs in μg mL –1 ) of compounds 6 , 11 , 12 and 13 against methicillin-sensitive Staphylococcus aureus , methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Staphylococcus aureus (VRSA) strains table ft1 table-wrap mode="anchored" t5 caption a7 Bacterial strains a Compounds/control antibiotics 6 11 12 13 Vancomycin Linezolid Staphylococcus epidermidis NRS101 4 0.5 0.25 0.06 2 1 Cephalosporin- resistant Streptococcus pneumoniae ATCC 51916 2 2 0.25 0.25 0.5 1 Methicillin- resistant Streptococcus pneumoniae ATCC 700677 1 1 0.25 0.125 1 1 Enterococcus faecalis ATCC 51299 (VRE) 4 8 4 2 32 1 Enterococcus faecium ATCC 700221 (VRE) 4 4 4 2 >64 1 Listeria monocytogenes ATCC 19111 2 2 0.5 0.125 0.5 0.5 Open in a separate window a See ESI for sources of bacterial strains. caption a8 The minimum inhibitory concentrations (MICs in μg mL –1 ) of compounds 6 , 11 , 12 and 13 against a panel of clinically important Gram-positive bacterial pathogens including Staphylococcus epidermidis , Streptococcus pneumoniae, Enterococcus faecalis , Enterococcus faecium and Listeria monocytogenes Compounds 6 , 11 , 12 and 13 are highly tolerable to human cell lines Selectivity towards prokaryotic cells is an essential attribute for any antibiotic candidate.

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Article Title: Epidemiology of Glycopeptide-Resistant Enterococci Colonizing High-Risk Patients in Hospitals in Johannesburg, Republic of South Africa

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Figure Lengend Snippet: Macrorestriction analysis of GRE isolates. Lanes 1 through 13, isolates from patients 1 through 13 as identified in Tables ​Tables11 and ​and2;2; lanes 14 to 19, E. faecium vanA (type A) isolated from S1 in 1997 and four different private hospitals in 1998; lane 20, E. faecium vanA (ATCC 51559); lanes 21 and 22, E. faecalis vanA isolates from S1 and S2; lane 23, E. faecalis vanA (ATCC 51299). The leftmost and rightmost lanes contain molecular size markers (PFGE marker 1 [λ ladder]; Boehringer GmbH, Mannheim, Germany).

Article Snippet: Broths exhibiting esculin hydrolysis were subcultured onto blood agar plates, which were then incubated for 24 to 48 h. The following strains were used as controls: E. casseliflavus ATCC 25788 ( vanC2 ; vancomycin MIC, 16 μg/ml; teicoplanin MIC, 0.5 μg/ml); E. faecalis ATCC 51575 ( vanB ; vancomycin MIC, >64 μg/ml; teicoplanin MIC, <0.12 μg/ml) and ATCC 51299 ( vanB ; vancomycin MIC, 2 μg/ml; teicoplanin MIC, <0.12 μg/ml); and E. faecium ATCC 19434 (vancomycin MIC, 0.25 μg/ml; teicoplanin MIC, <0.12 μg/ml) and ATCC 51559 ( vanA ; vancomycin MIC, 64 μg/ml; teicoplanin MIC, 64 μg/ml).

Techniques: Isolation, Marker