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Sultana, Najma,Arayne, Muhammad Saeed,Rizvi, Syeda Bushra Shakeb,Mesaik, Muhammad Ahmed Korean Chemical Society 2009 Bulletin of the Korean Chemical Society Vol.30 No.10
In present work an attempt was made to synthesize various analogues of levofloxacin by introducing new functionality at carboxylic group position via nucleophilic substitution reaction. For this purpose the carboxylic group at C-6 was esterified and later subjected to nucleophilic attack at the carbonyl carbon by various aromatic amines. Structure of the analogues was confirmed by different techniques i.e. IR, $^1H$ NMR and mass spectrometry. The antibacterial activity of the derivatives was also assessed and compared with the parent against a series of Gram-positive and Gramnegative bacteria. A synergistic as well as antagonistic behavior was observed in these derivatives. Additionally unlike levofloxacin, the derivatives were also found to modulate oxidative burst response of phagocytes exhibiting moderate to significant inhibitory activity.
Najma Sultana,Muhammad Saeed Arayne,Syeda Bushra Shakeb Rizvi,Muhammad Ahmed Mesaik 대한화학회 2009 Bulletin of the Korean Chemical Society Vol.30 No.10
In present work an attempt was made to synthesize various analogues of levofloxacin by introducing new functionality at carboxylic group position via nucleophilic substitution reaction. For this purpose the carboxylic group at C-6 was esterified and later subjected to nucleophilic attack at the carbonyl carbon by various aromatic amines. Structure of the analogues was confirmed by different techniques i.e. IR, 1H NMR and mass spectrometry. The antibacterial activity of the derivatives was also assessed and compared with the parent against a series of Gram-positive and Gramnegative bacteria. A synergistic as well as antagonistic behavior was observed in these derivatives. Additionally unlike levofloxacin, the derivatives were also found to modulate oxidative burst response of phagocytes exhibiting moderate to significant inhibitory activity.
Synthesis and Biological Evaluations of Enoxacin Carboxamide Derivatives
M. Saeed Arayne,Najma Sultana,Urooj Haroon,M. Ahmed Mesaik,Muhammad Asif 대한약학회 2009 Archives of Pharmacal Research Vol.32 No.7
The present work deals with the synthesis of various enoxacin analogues via nucleophilic substitution of 3- carboxylic acid moiety of the drug by aromatic amines. The free carboxylic group was utilized in the formation of amides and the effect of functional group exchange on different biological activities of the parent was evaluated. The structure of these derivatives was established by various spectroscopic techniques and mass spectrometry. The derivatives were evaluated as antibacterial agents against a series of Gram-positive and Gram-negative bacteria whereby some of them displayed considerably improved antimicrobial profile against Gramnegative test strains. Additionally unlike enoxacin, the derivatives were also found to modulate oxidative burst response of phagocytes exhibiting moderate to significant inhibitory activity.