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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, Characterization and Biological Evaluations of Ciprofloxacin Carboxamide Analogues
Najma Sultana,Muhammad Saeed Arayne,Syeda Bushra Shakeb Rizvi,Urooj Haroon 대한화학회 2011 Bulletin of the Korean Chemical Society Vol.32 No.2
Present work comprises of synthesis various analogues of ciprofloxacin by introducing new functionality at carboxylic group position via ester aminolysis reaction. For this purpose the carboxylic group at C-3 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, ^(1)H NMR and mass spectrometry. The antibacterial activity of the derivatives was also assessed with the parent against a series of Gram-positive and Gram-negative bacteria. The synthesized compounds showed diverse antimicrobial profile among which most compounds possessed a comparable or better activity in comparison to the ciprofloxacin. Additionally unlike ciprofloxacin, some of the derivatives were also found to show antifungal activity.
Synthesis, Characterization and Biological Evaluations of Ciprofloxacin Carboxamide Analogues
Sultana, Najma,Arayne, Muhammad Saeed,Rizvi, Syeda Bushra Shakeb,Haroon, Urooj Korean Chemical Society 2011 Bulletin of the Korean Chemical Society Vol.32 No.2
Present work comprises of synthesis various analogues of ciprofloxacin by introducing new functionality at carboxylic group position via ester aminolysis reaction. For this purpose the carboxylic group at C-3 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 with the parent against a series of Gram-positive and Gram-negative bacteria. The synthesized compounds showed diverse antimicrobial profile among which most compounds possessed a comparable or better activity in comparison to the ciprofloxacin. Additionally unlike ciprofloxacin, some of the derivatives were also found to show antifungal activity.
M. Saeed Arayne,Najma Sultana,M. Hashim Zuberi,Syeda Bushra Shakeb Rizvi,Urooj Haroon 대한약학회 2010 Archives of Pharmacal Research Vol.33 No.12
The present study was designed to help develop new agents with better antimicrobial profiles. Specifically, we focused on modification of the basic structure of ofloxacin by introducing new functionality at its C3 position. For this purpose, the carboxylic group at the C3 position of ofloxacin was replaced by an amide group through an ester aminolysis reaction. The structure of these derivatives was established by various analytical techniques i.e., IR, 1H-NMR, 13CNMR CHNS elemental analysis and mass spectrometry. The antibacterial activity of ofloxacin and its derivatives against ten different Gram-positive and Gram-negative microorganisms was studied using a disk susceptibility method. These compounds were further tested for their activity against various fungi and compared to ofloxacin. The synthesized compounds showed diverse antimicrobial profiles. Among them, a few compounds possessed a comparable or better activity in comparison to the reference drug.