ChemInform Abstract: Dialkyl (1,2‐Epoxy‐3‐oxoalkyl)phosphonates as Synthons for Heterocyclic Carbonyl Compounds: Synthesis of Acy1‐Substituted Thiazoles, Indolizines, Imidazo[1,2‐a]‐pyridines and Imidazol[1,2‐a]pyrimidines.

Oehler, E.; El‐Badawi, Mahmoud A.; Zbiral, E.

doi:10.1002/chin.198603268

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2014

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“…The reaction mixtures were heated at reflux for 12–24 h. After evaporation of solvent under reduced pressure, the brown residues were collected and purified by silica gel flash chromatography, using hexane-ethyl acetate (9:1), to yield compounds 4a-i in the desired purity. Compounds 4a 16 and 4b 17 are previously reported. Characterizations of compounds 4c-i are listed in SI.…”

Section: Methodsmentioning

confidence: 93%

Discovery and Characterization of Potent Thiazoles versus Methicillin- and Vancomycin-Resistant Staphylococcus aureus

et al. 2014

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Methicillin- and vancomycin-resistant Staphylococcus aureus (MRSA & VRSA) infections are growing global health concerns. Structure-activity-relationships of phenylthiazoles as a new antimicrobial class have been addressed. We present 10 thiazole derivatives that exhibit strong activity against 18 clinical strains of MRSA and VRSA with acceptable PK profile. Three derivatives revealed an advantage over vancomycin by rapidly eliminating MRSA growth within six hours and no derivatives are toxic to HeLa cells at a concentration of 11 μg/mL.

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Section: Methodsmentioning

confidence: 93%