- Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure
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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.
- Suzuki, Hideyuki,Utsunomiya, Iwao,Shudo, Koichi,Fujimura, Takaji,Tsuji, Masakatsu,Kato, Issei,Aoki, Toshiaki,Ino, Akira,Iwaki, Tsutomu
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supporting information
p. 1074 - 1078
(2013/12/04)
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- OXAZOLIDINONE DERIVATIVE HAVING FUSED RING
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The present invention provides a novel antimicrobial drug comprising an oxazolidinone derivative of the formula (I): or a pharmaceutically acceptable salt or solvate thereof; wherein ring A is ring B is a benzene ring optionally substituted with lower alkyl; ring C is an optionally substituted six-membered heterocycle containing at least one nitrogen atom and one to three double bond(s) in the ling wherein the atom at the point of attachment to ring B is a carbon atom; ring D is an optionally substituted five-membered ring containing one or two double bond(s) in the ring; A1 and A2 are independently nitrogen or carbon; m is 0 or 1; R represents H, —NHC(═O)RA, —NHC(═S)RA, —NH-het1, —O-het1, —S-het1, —S(═O)-het1, —S(═O)2-het1, het2, —CONHRA, —OH, lower alkyl, lower alkoxy or lower alkenyl; and het1 and het2 are independently a heterocyclic group; with the proviso that the fused ring C-D is not
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