1202702-15-5Relevant academic research and scientific papers
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure
Suzuki, Hideyuki,Utsunomiya, Iwao,Shudo, Koichi,Fujimura, Takaji,Tsuji, Masakatsu,Kato, Issei,Aoki, Toshiaki,Ino, Akira,Iwaki, Tsutomu
supporting information, p. 1074 - 1078 (2013/12/04)
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.
OXAZOLIDINONE DERIVATIVE HAVING FUSED RING
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Page/Page column 64, (2011/05/05)
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
