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      • KCI등재

        Synthesis, Characterization and Biological Evaluation of a Series of Levofloxacin Carboxamide Analogues

        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.

      • SCOPUSKCI등재

        Synthesis, Characterization and Biological Evaluation of a Series of Levofloxacin Carboxamide Analogues

        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.

      • KCI등재

        Ustekinumab for the treatment of refractory pediatric Crohn’s disease: a single-center experience

        ( Alexandra Cohen ),( Najma Ahmed ),( Ana Sant’anna ) 대한장연구학회 2021 Intestinal Research Vol.19 No.2

        Background/Aims: Despite the well-established efficacy of tumor necrosis factor (TNF) antagonists as treatment options for Crohn’s disease, many pediatric patients need a change in therapy due to adverse events and loss of response, highlighting the necessity for medications with a different mechanism of action. Ustekinumab has been shown to be effective in inducing clinical remission in some adults with disease refractory to anti-TNF agents, however, minimal data exists in the pediatric population. Methods: We conducted a retrospective chart review of 11 pediatric patients receiving ustekinumab, specifically extracting baseline data, information on prior treatment and response, indications for starting ustekinumab, clinical information, and laboratory parameters pre- and post-therapy. Clinical response was defined as a decrease in abbreviated Pediatric Crohn’s Disease Activity Index score. Results: Patients ranged from 12 to 17 years of age upon initiation of treatment with ustekinumab. Five of 11 patients demonstrated a clinical response. Among these patients, 2 remained in clinical remission, while the remaining 3 experienced a secondary loss of response. The other 6 patients were primary nonresponders who either remained unwell or demonstrated slight clinical worsening. All patients who clinically responded to ustekinumab and had an initially elevated CRP experienced complete normalization of their values. Mucosal healing was seen on endoscopy in 1 responder, with 2 other patients showing endoscopic improvement. Conclusions: These results demonstrate for the first time that ustekinumab has the potential to induce not only clinical and biochemical remission, but also endoscopic improvement, in the pediatric population. Future research is needed to determine factors that influence response to therapy. (Intest Res 2021;19:217-224)

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        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.

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