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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.
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.
Method Development of Verapamil in Presence of NSAIDs using RP-HPLC Technique
Sultana, Najma,Arayne, M. Saeed,Waheed, Abdul Korean Chemical Society 2011 Bulletin of the Korean Chemical Society Vol.32 No.7
Verapamil is a calcium channel blocker and is classified as a class IV anti-arrhythmic agent. It is used in the control of supra ventricular tachyarrhythmias, and in the management of classical and variant angina pectoris. It is also used in the treatment of hypertension and used as an important therapeutic agent for angina pectoris, ischemic heart disease, hypertension and hypertrophic cardiomyopathy. Verapamil commonly co-administered with NSAIDs (non-steroidal anti-inflammatory drugs) i.e. diclofenac sodium, flurbiprofen, Ibuprofen, mefanamic acid and meloxicam. A simple and rapid RP-HPLC method for simultaneous determination and quantification of verapamil and NSAIDs was developed and validated. The mobile phase constituted of acetonitrile: water (55:45) whose pH was adjusted at 2.7 and pumped at a flow rate of 2.0 mL $min^{-1}$ at 230 nm. The proposed method is simple, precise, accurate, low cost and least time consuming for the simultaneous determination of verapamil and NSAIDs which can be effectively applied for the analysis of human serum.
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.
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.
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.
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.
Method Development of Verapamil in Presence of NSAIDs using RP-HPLC Technique
Najma Sultana,M. Saeed Arayne,Abdul Waheed 대한화학회 2011 Bulletin of the Korean Chemical Society Vol.32 No.7
Verapamil is a calcium channel blocker and is classified as a class IV anti-arrhythmic agent. It is used in the control of supra ventricular tachyarrhythmias, and in the management of classical and variant angina pectoris. It is also used in the treatment of hypertension and used as an important therapeutic agent for angina pectoris,ischemic heart disease, hypertension and hypertrophic cardiomyopathy. Verapamil commonly co-administered with NSAIDs (non-steroidal anti-inflammatory drugs) i.e. diclofenac sodium, flurbiprofen, Ibuprofen,mefanamic acid and meloxicam. A simple and rapid RP-HPLC method for simultaneous determination and quantification of verapamil and NSAIDs was developed and validated. The mobile phase constituted of acetonitrile: water (55:45) whose pH was adjusted at 2.7 and pumped at a flow rate of 2.0 mL min^−1 at 230 nm. The proposed method is simple, precise, accurate, low cost and least time consuming for the simultaneous determination of verapamil and NSAIDs which can be effectively applied for the analysis of human serum.