- Oxazolidinone compound containing piperazine hydrazone structure
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The invention discloses an oxazolidinone compound containing a piperazine hydrazone structure. The oxazolidinone compound comprises a compound shown as a general formula (I), or stereisomer thereof, or pharmaceutically-acceptable salt thereof, or solvate thereof or prodrug thereof, wherein R1 is hydrogen, fluorine, chlorine or trifluoromethyl, R2 is -NHCOCH3 or -OH, R3 is Ar which is C5-C10 aryl substituted by any 1-3 R4 and heteroaryl, and R4 is hydrogen, hydroxyl, halogen, nitro, amino, cyan, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkyl substituted by hydroxyl, amino or halogen, C1-C6 alkoxy substituted by hydroxyl, amino or halogen, amino substituted by mono- or bi-(C1-C6 alkyl), C1-C6 alkyl amido, free, salty, esterified and amidated hydroxyl, C1-C6 alkyl sulfinyl, C1-C6 alkyl sulfonyl, C1-C6 alkyl acyl and carbamoyl. The oxazolidinone compound can be used for preparing drug for treating microbial infection.
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Paragraph 0091; 0092
(2017/09/02)
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- Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents
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Novel oxazolidinone antibacterials bearing a variety of 3-indolylglyoxamide substituents have been explored in an effort to improve the spectrum and potency of this class of agents. A subclass of this series was also made with the diversity at C-5 terminus. These derivatives have been screened against a panel of clinically relevant Gram-positive pathogens and fastidious Gram-negative organisms. Several analogs in this series were identified with in vitro activity superior to linezolid (MIC = 0.25-2 μg/mL). Compounds 10a, 10c, 10e and 10f displayed activity against linezolid resistant Gram-positive organisms (MIC = 2-4 μg/mL). Selected oxazolidinones were evaluated for in vivo efficacy against a mouse systemic infection model.
- Takhi, Mohamed,Singh, Gurpreet,Murugan,Thaplyyal, Nirvesh,Maitra, Soma,Bhaskarreddy,Amarnath,Mallik, Arundhuti,Harisudan,Trivedi, Ravi Kumar,Sreenivas,Selvakumar,Iqbal, Javed
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scheme or table
p. 5150 - 5155
(2009/05/26)
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- Synthesis and SAR of novel oxazolidinones: Discovery of ranbezolid
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Novel oxazolidinones were synthesized containing a number of substituted five-membered heterocycles attached to the 'piperazinyl-phenyl-oxazolidinone' core of eperezolid. Further, the piperazine ring of the core was replaced by other diamino-heterocycles.
- Das, Biswajit,Rudra, Sonali,Yadav, Ajay,Ray, Abhijit,Raja Rao,Srinivas,Soni, Ajay,Saini, Suman,Shukla, Shalini,Pandya, Manisha,Bhateja, Pragya,Malhotra, Sunita,Mathur, Tarun,Arora,Rattan, Ashok,Mehta, Anita
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p. 4261 - 4267
(2007/10/03)
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- NOVEL ANTIBACTERIAL AGENTS
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The present invention provides novel compounds of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and phar
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