- RETRACTED ARTICLE: Design, synthesis of novel oxazolidino-amides/sulfonamides conjugates and their impact on antibacterial activity
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Abstract: In view of generating new compounds for future drug development, we have synthesized oxazolidinones library of aryl amides and aryl sulfonamide derivatives. These compounds were screened in vitro against panel of susceptible and resistant Gram-p
- Bharath, Yarlagadda,Alugubelli, Gopi Reddy,Sreenivasulu, Reddymasu,Rao, Mandava. V. Basaveswara
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p. 457 - 468
(2018/02/09)
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- Synthesis and antibacterial activity of novel 5-(4-methyl-1H-1,2,3-triazole) methyl oxazolidinones
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A series of 5-(4-methyl-1,2,3-triazole)methyl oxazolidinones were synthesized and tested for their antibacterial activity against a panel of Gram-positive and Gram-negative clinical isolates in comparison with linezolid and vancomycin. Most of the compounds demonstrated strong to moderate in vitro antibacterial activity against susceptible and resistant Gram-positive pathogenic bacteria. Antibacterial activity varied with substitutions at the phenyl C4 position with bulky alkylcarbonyl and alkoxycarbonyl substitutions on the piperazine N4 being detrimental to antibacterial activity. Whereas the presence of the 4-methyl-1,2,3-triazole moiety in the acyl-piperazine containing analogs resulted in increased protein binding, and decreased antibacterial activity particularly against Streptococcus pneumoniae strains.
- Phillips, Oludotun A.,Udo, Edet E.,Abdel-Hamid, Mohammed E.,Varghese, Reny
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scheme or table
p. 3217 - 3227
(2009/12/04)
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- Synthesis and structure-antibacterial activity of triazolyl oxazolidinones containing long chain acyl moiety
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A series of new piperazinyl 5-triazolylmethyl oxazolidinones containing long chain acyl group at the piperazine N-4-position were synthesized and evaluated against a panel of standard and clinical isolates of Gram-positive and Gram-negative bacteria. Deri
- Phillips, Oludotun A.,Udo, Edet E.,Samuel, Santhosh M.
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p. 1095 - 1104
(2008/09/20)
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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 antibacterial activity of novel oxazolidinones bearing N-hydroxyacetamidine substituent
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Novel oxazolidinone antibacterials containing N-hydroxyacetamidine moiety are synthesized with the diversity at C-5 terminus. These compounds have been evaluated against a panel of clinically relevant Gram-positive and Gram-negative pathogens. Most of the
- Takhi, Mohamed,Murugan,Munikumar,Bhaskarreddy,Singh, Gurpreet,Sreenivas,Sitaramkumar,Selvakumar,Das,Trehan, Sanjay,Iqbal, Javed
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p. 2391 - 2395
(2007/10/03)
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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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