Synthesis and structure-activity studies of novel benzocycloheptanone oxazolidinone antibacterial agents.
Pfizer Global Research and Development, 2800 Plymouth Road, Ann Arbor, MI 48105, USA.Bioorganic & Medicinal Chemistry Letters (Impact Factor: 2.34). 11/2006; 16(20):5392-7. DOI:10.1016/j.bmcl.2006.07.064
ABSTRACT We describe a novel class of benzocycloheptanone derived oxazolidinone antibacterial agents. The synthesis and antibacterial activities with structure variation is discussed.
- SourceAvailable from: Nagatoshi Nishiwaki[show abstract] [hide abstract]
ABSTRACT: beta-formyl-beta-nitroenamines possess both an electrophilic formyl group and a nucleophilic amino group and, therefore, serve as C3N1 building blocks having a nitro group to afford nitropyridones and aminonitropyridines with a functional group at the 3-position. Upon treatment with malonic acid derivatives or beta-keto esters, nitropyridones were obtained, whereas reactions with functionalized acetonitriles afford aminonitropyridines, via a formal transfer of an alkyl group from the ring nitrogen to the imino group. These procedures provide practical and useful methods for preparation of heterocycles with a nitro group.Organic & Biomolecular Chemistry 02/2009; 7(2):325-34. · 3.57 Impact Factor
Article: New oxazolidinones.[show abstract] [hide abstract]
ABSTRACT: Due to the emergence of resistance to known antibiotics to various organisms, for example, Staphylococcus, Streptococcus, Enterococci, and Pseudomonas there is a renewed interest in the discovery of new antibacterials. Oxazolidinones, totally synthetic class of novel antibacterials, possess activity against drug-resistant Gram-positive pathogens, especially MRSA. Linezolid, the first approved drug from this class, has shown a great promise in saving lives of many patients by acting against drug-resistant Gram-positive organisms. However, its use is somewhat limited because of its myelotoxicity when used long term (>21 days). Various research groups are active in this area either to improve myelotoxicity profile of linezolid or to expand the spectrum of activity of linezolid. In spite of active research in this area, the discovery of an oxazolidinone possessing improved myelotoxicity compared to linezolid, linezolid-like efficacy, and PK remains challenging.Current Opinion in Microbiology 10/2007; 10(5):454-60. · 8.23 Impact Factor
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