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1.
Arch Pharm (Weinheim) ; : e1900294, 2020 Jan 02.
Artigo em Inglês | MEDLINE | ID: mdl-31894862

RESUMO

A series of (3-benzyl-5-hydroxyphenyl)carbamates were evaluated as new antibacterial agents. Several compounds showed potent inhibitory activity against sensitive and drug-resistant Gram-positive bacteria. The compounds are ineffective against all tested Gram-negative bacteria. The structure of the ester group exerted a profound effect on antibacterial activity. 4,4-Dimethylcyclohexanyl carbamate 6h exhibited the most potent inhibitory activity against the standard and clinically isolated Staphylococcus aureus, Staphylococcus epidermidis, and Enterococcus faecalis (minimum inhibitory concentration = 4-8 µg/ml) strains. The preliminary experimental evidence indicated that these carbamates target the bacterial cell wall and share a similar mechanism of action with vancomycin.

3.
Org Lett ; 21(23): 9742-9746, 2019 Dec 06.
Artigo em Inglês | MEDLINE | ID: mdl-31725305

RESUMO

An enantioselective conjugate addition of ethylene sulfonyl fluorides to 3-amido-2-oxindoles has been developed. Quinine-derived squaramides were identified as efficient catalysts. A series of spirocyclic oxindole sultams were prepared with excellent yields and enantioselectivities. A reaction mechanism via bifunctional activation was proposed.

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