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Biomedical subjects

G D Cuny

Publications and source records attributed to G D Cuny.

3 recordsLinked to original sources

Potent in vitro methicillin-resistant Staphylococcus aureus activity of 2-(1H-indol-3-yl)quinoline derivatives.

A novel structural class of antibacterials, 2-(1H-indol-3-yl)quinolines, effective against methicillin-resistant Staphylococcus aureus (MRSA), was discovered from a combinatorial library. A structure-activity relationship (SAR) study was conducted to determine the pharmacophore and increase the potency of these compounds. Compounds were prepared that had minimum inhibitory concentrations (MICs) < 1.0 microg/mL against MRSA and retained activity against two strains of glycopeptide intermediate-resistant S. aureus (GISA).

Anti-Bacterial Agents↗

Ring opening cross-metathesis on solid support: a combinatorial library synthesis of highly functionalized cyclopentanes.

Ruthenium catalyzed ring opening cross-metathesis of resin-bound bicyclic alkenes with terminal aryl olefins was utilized for the construction of a combinatorial library containing highly functionalized cyclopentane derivatives. The technology described herein represents a convergent method for the diastereospecific synthesis of unique cyclopentane molecular scaffolds useful for exploratory medicinal chemistry.

Chemistry, Organic↗