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- W2023576255 abstract "Many attempts have been made to prepare analogs of 4-quinolone antibacterial agents bearing novel ring systems, which might retain the favorable properties of these widely used antibacterial agents and at the same time increase activity against multidrug-resistant bacteria, streptococci, and anaerobic microorganisms. One such attempt involved bioisosteric exchange of the 1-N atom and 4a-C atom of naphthyridones, quinolones, and benzoxazines to produce a family of highly active pyridopyrimidines, quinolizines, and ofloxacin bioisosteres. These new antibacterial agents have been named collectively as the 2-pyridones. Many hundreds of 2-pyridones have been synthesized and evaluated in vitro and in vivo, and selected members are advancing toward human clinical trials. Preparation of these bioisosteres required the development of enabling chemistry, as previous methods were unsuccessful in producing the needed core structures. This review compares the structure-activity relationships of these agents with known trends among 4-quinolones, from which it is seen that there are many parallels, but also some significant departures as well. Generally, 2-pyridones are more highly active in vitro and in vivo and more water soluble than comparable 4-quinolones. These properties are posited to arise from electronic and conformational alternations in these new substances. Selected members show excellent pharmacodynamic properties, justifying the view that this is a very promising new class of totally synthetic antibacterial agents." @default.
- W2023576255 created "2016-06-24" @default.
- W2023576255 creator A5058040686 @default.
- W2023576255 creator A5065112951 @default.
- W2023576255 creator A5066887020 @default.
- W2023576255 date "2000-01-01" @default.
- W2023576255 modified "2023-10-14" @default.
- W2023576255 title "The 2-pyridone antibacterial agents: bacterial topoisomerase inhibitors" @default.
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- W2023576255 doi "https://doi.org/10.1002/1098-1128(200007)20:4<231::aid-med1>3.0.co;2-n" @default.
- W2023576255 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/10861727" @default.
- W2023576255 hasPublicationYear "2000" @default.
- W2023576255 type Work @default.