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Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.

ABSTRACT: Novel oxazolidinone analogues bearing a condensed heteroaromatic ring as the C-ring substructure were synthesized as candidate antibacterial agents. Analogues 16 and 21 bearing imidazo[1,2-a]pyridine and 18 and 23 bearing [1,2,4]triazolo[1,5-a]pyridine as the C-ring had excellent in vitro antibacterial activities against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecalis (VRE), and penicillin-resistant Streptococcus pneumoniae (PRSP). They also showed promising therapeutic effects in a mouse model of lethal infection. Preliminary safety data (inhibitory effects on cytochrome P450 isoforms and monoamine oxidases) were satisfactory. Further evaluation of 18 and 23 is ongoing.

SUBMITTER: Suzuki H

PROVIDER: S-EPMC4027242 | biostudies-literature | 2013 Nov

REPOSITORIES: biostudies-literature

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Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.

Suzuki Hideyuki H Utsunomiya Iwao I Shudo Koichi K Fujimura Takaji T Tsuji Masakatsu M Kato Issei I Aoki Toshiaki T Ino Akira A Iwaki Tsutomu T

ACS medicinal chemistry letters 20130922 11

Novel oxazolidinone analogues bearing a condensed heteroaromatic ring as the C-ring substructure were synthesized as candidate antibacterial agents. Analogues 16 and 21 bearing imidazo[1,2-a]pyridine and 18 and 23 bearing [1,2,4]triazolo[1,5-a]pyridine as the C-ring had excellent in vitro antibacterial activities against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecalis (VRE), and penicillin-resistant Streptococcus pneumoniae (PRSP). They also showed ...[more]

PMID: 24900607

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