5997-01-3Relevant articles and documents
Optimization of biaryloxazolidinone as promising antibacterial agents against antibiotic-susceptible and antibiotic-resistant gram-positive bacteria
Wu, Yachuang,Ding, Xiudong,Yang, Yifeng,Li, Yingxiu,Qi, Yinliang,Hu, Feng,Qin, Mingze,Liu, Yajing,Sun, Lu,Zhao, Yanfang
, (2019/10/23)
We previously discovered a series of novel biaryloxazolidinone analogues bearing a hydrazone moiety with potent antibacterial activity. However, the most potent compound OB-104 exhibited undesirable chemical and metabolic instability. Herein, novel biaryloxazolidinone analogues were designed and synthesized to improve the chemical and metabolic stability. Compounds 6a-1, 6a-3, 14a-1, 14a-3 and 14a-7 showed significant antibacterial activity against the tested Gram-positive bacteria as compared to radezolid and linezolid. Further studies indicated that most of them exhibited improved water solubility and chemical stability. Compound 14a-7 had MIC values of 0.125–0.25 μg/mL against all tested Gram-positive bacteria, and showed excellent antibacterial activity against clinical isolates of antibiotic-susceptible and antibiotic-resistant bacteria. Moreover, it was stable in human liver microsome. From a safety viewpoint, it showed non-cytotoxic activity against hepatic cell and exhibited lower inhibitory activity against human MAO-A compared to linezolid. The potent antibacterial activity and all these improved drug-likeness properties and safety profile suggested that compound 14a-7 might be a promising drug candidate for further investigation.
NEW DRUGS WITH ANTICHOLESTATIC ACTIVITY
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Page/Page column 25, (2009/03/07)
New compounds belonging to the structural formula (I) are described. formula (I) in which R1, R2, A, Y and X are specified in the description, useful in the treatment of cholestasis and substantially devoid of antibacterial activity. The synthesis process of said compounds, the pharmaceutical compositions containing them and their use in therapy are also described.
ALPHA-MERCAPTOMETHYL-BENZENE PROPANAMIDES, PHARMACEUTICAL COMPOSITIONS AND USE
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, (2008/06/13)
Novel α-mercaptomethyl-benzene propanamides of the formula STR1 wherein R 1 is selected from the group consisting of hydrogen and STR2 R 1 ' is selected from the group consisting of alkyl of 1 to 5 carbon atoms and aryl optionally substituted with at least one member of the group consisting of--OH,--NO 2, halogen and alkyl and alkoxy of 1 to 5 carbon atoms, X and X' are individually selected from the group consisting of hydrogen, alkyl and alkoxy of 1 to 5 carbon atoms,--OH, halogen and--CF 3, R 2 is selected from the group consisting of pyrrolidinyl, morpholinyl, piperidinyl, piperazinyl, tetrahydrothiazinyl and hexahydroazepinyl, all optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms,--OH,--NO. sub.2,--CF 3, halogen and acyl of an organic carboxylic acid of 1 to 7 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having analgesic activity, antidepression and anxiolytic properties.