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Discovery of isoxazolinone antibacterial agents. Nitrogen as a replacement for the stereogenic center found in oxazolidinone antibacterials.

A series of potential antimicrobial derivatives possessing bioisosteric replacements for the central oxazolidinone ring found in oxazolidinone antibacterials have been prepared. The design concept involved replacement of the requisite sp(3)-hybridized stereogenic center found at the 5-position of the oxazolidinone with a nitrogen atom. The synthesis and antibacterial activity of three such ring systems, the benzisoxazolinones, pyrroles, and isoxazolinones is described.

Date de publication
20 septembre 2004
Chercheur(euse)s
Snyder LB, Meng Z, Mate R, D'Andrea SV, Marinier A, Quesnelle CA, Gill P, DenBleyker KL, Fung-Tomc JC, Frosco M, Martel A, Barrett JF, Bronson JJ
Référence PubMed
Bioorg. Med. Chem. Lett. 2004;14(18):4735-9
ID PubMed
15324898
Affiliation
Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. lawrence.snyder@bms.com