Syntheses and biological studies of novel spiropiperazinyl oxazolidinone antibacterial agents using a spirocyclic diene derived acylnitroso Diels-Alder reaction.

Bioorganic & Medicinal Chemistry
Cheng JiMarvin J Miller

Abstract

Several novel oxazolidinone antibiotics with a spiropiperazinyl substituent at the 4'-position of the phenyl ring were synthesized through nitroso Diels-Alder chemistry and the in vitro antibacterial activities were evaluated against various Gram-positive bacteria (Bacillus subtilis, Staphylococcus aureus, Enterococcus faecalis), Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and mycobacteria (Mycobacterium vaccae, Mycobacterium tuberculosis). Analogs (8a and 12) were active against selected drug resistant microbes, like methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE) and had no mammalian toxicity in a Hep-2 cellular assay (CC(50) >100 μM).

References

Jan 1, 1988·Antimicrobial Agents and Chemotherapy·A L Barry
Apr 1, 1988·Antimicrobial Agents and Chemotherapy·H C NeuN X Chin
Oct 31, 2002·The Journal of Antimicrobial Chemotherapy·Cressida AucklandAlan P Johnson
Nov 25, 2004·Antimicrobial Agents and Chemotherapy·Mahesh V PatelPeter C Appelbaum
Aug 5, 2005·Journal of Medicinal Chemistry·Noel J de SouzaHabil F Khorakiwala
Sep 20, 2006·Antimicrobial Agents and Chemotherapy·Jamela SeedatHany Sahly

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Citations

Jan 21, 2017·Chemical Reviews·Misal Giuseppe Memeo, Paolo Quadrelli

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