Microwave assisted synthesis of some hybrid molecules derived from norfloxacin and investigation of their biological activities

Menteşe, Meltem; Bayrak, Hacer; Uygun, Yıldız; Mermer, Arif; Ülker, Serdar; Karaoğlu, Şengül Alpay; Demirbaş, Neslihan

doi:10.1016/j.ejmech.2013.06.045

Cited by 69 publications

(48 citation statements)

References 56 publications

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“…Urease is an enzyme that catalyses the hydrolysis of urea into carbon dioxide and ammonia. The production of ammonia was measured by the indophenol method and used to determine the urease inhibitory activity [29]. The percentage inhibition was calculated from the formula: % Inhibition = [(OD control − OD test )/(OD control ) × 100].…”

Section: Anti-xanthine Oxidase and Anti-urease Activity Of Pyrus Elaementioning

confidence: 99%

Investigation of a wild pear species (Pyrus elaeagnifoliasubsp.ElaeagnifoliaPallas) from Antalya, Turkey: polyphenol oxidase properties and anti-xanthine oxidase, anti-urease, and antioxidant activity

Baltaş

2016

International Journal of Food Properties

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Polyphenol oxidase (PPO) properties and anti-xanthine oxidase, anti-urease and antioxidant activity were investigated in Pyrus elaeagnifolia subsp. elaeagnifolia Pallas harvested from Antalya, Turkey. Optimum pH and temperature were 7.0 and 30 °C, respectively. Selected kinetic properties of PPO was evaluated.The K m and V max values, using 4-methylcatechol as substrate, were calculated as 3.57 mM and 4781 U/mg protein, respectively. IC 50 values ranged from 0.0036 to 4.0231 mM against sodium metabisulphite, ascorbic acid, sodium azide and benzoic acid, while ascorbic acid was the strongest inhibitor. Aquatic extracts of the samples exhibited strong antioxidant capacity and substantial xanthine oxidase and urease inhibition, with IC 50 values of 20.75 ± 0.11 and 2.97 ± 0.09 mg/mL, respectively.

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Section: Anti-xanthine Oxidase and Anti-urease Activity Of Pyrus Elaementioning

confidence: 99%

Investigation of a wild pear species (Pyrus elaeagnifoliasubsp.ElaeagnifoliaPallas) from Antalya, Turkey: polyphenol oxidase properties and anti-xanthine oxidase, anti-urease, and antioxidant activity

Baltaş

2016

International Journal of Food Properties

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“…However, the most successful compounds developed are based on modifications at C-7, considering that the nature of the substituent in this position controlled the spectrum, level of antibacterial activity, cell permeability, solubility, and pharmacokinetics. Molecules in clinical use have substituents such as piperazinyl, pyrrolidinyl, piperidinyl, pyridyl, and azabicyclic moieties in position C-7 [4,5,6,7] (Fig. 1).…”

Section: Introductionmentioning

confidence: 99%

In vitro Antibacterial Activity of 7-Substituted-6-Fluoroquinolone and 7-Substituted-6,8-Difluoroquinolone Derivatives

Leyva‐Ramos

Loera²,

Cardoso‐Ortiz³

2017

Chemotherapy

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Background: Fluoroquinolones are widely prescribed synthetic antimicrobial agents. Quinolones act by converting their targets, gyrase and topoisomerase IV, into toxic enzymes that fragment the bacterial chromosome; the irreversible DNA damage eventually causes the killing of bacteria. Thorough knowledge of the structure-activity relationship of quinolones is essential for the development of new drugs with improved activity against resistant strains. Methods: The compounds were screened for their antibacterial activity against 4 representing strains using the Kirby-Bauer disk diffusion method. Minimal inhibitory concentration (MIC) was determined by measuring the diameter of the inhibition zone using concentrations between 250 and 0.004 μg/mL. Results: MIC of derivatives 2, 3, and 4 showed potent antimicrobial activity against gram-positive and gram-negative bacteria. The effective concentrations were 0.860 μg/mL or lower. MIC for compounds 5-11 were between 120 and 515 μg/mL against Escherichia coli and Staphylococcus aureus, and substituted hydrazinoquinolones 7-10 showed poor antibacterial activity against gram-positive and gram-negative bacteria compared with other quinolones. Conclusion: Compounds obtained by modifications on C-7 of norfloxacin with the acetylated piperazinyl, halogen atoms, and substituted hydrazinyl showed good in vitro activity - some even better than the original compound.

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“…Moreover, increasing bulk at C-7 position is tolerated (12). Thus, much effort has been made on the structural modification of C-7 position in quinolones by incorporating several bioactive moieties including macrolides (13,14), oxazolidinones (15), triazoles (16), 5-(nitroaryl)-1,3,4-thiadiazoles (17,18) and sulfonamides (19,20). This led to obtaining quinolone hybrids as a new class of antimicrobial agents (21).…”

mentioning

confidence: 98%

Design, Synthesis, Antibacterial Evaluation and Docking Study of Novel 2‐Hydroxy‐3‐(nitroimidazolyl)‐propyl‐derived Quinolone

Xing

Cheng

et al. 2014

Chem Biol Drug Des

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A novel series of 2-hydroxy-3-(nitroimidazolyl)-propyl-derived quinolones 6a-o were synthesized and evaluated for their in vitro antibacterial activity. Most of the target compounds exhibited potent activity against Gram-positive strains. Among them, moxifloxacin analog 6n displayed the most potent activity against Gram-positive strains including S. epidermidis (MIC = 0.06 μg/mL), MSSE (MIC = 0.125 μg/mL), MRSE (MIC = 0.03 μg/mL), S. aureus (MIC = 0.125 μg/mL), MSSA (MIC = 0.125 μg/mL), (MIC = 2 μg/mL). Its activity against MRSA was eightfold more potent than reference drug gatifloxacin. Finally, docking study of the target compound 6n revealed that the binding model of quinolone nucleus was similar to that of gatifloxacin and the 2-hydroxy-3-(nitroimidazolyl)-propyl group formed two additional hydrogen bonds.

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Microwave assisted synthesis of some hybrid molecules derived from norfloxacin and investigation of their biological activities

Cited by 69 publications

References 56 publications

Investigation of a wild pear species (Pyrus elaeagnifoliasubsp.ElaeagnifoliaPallas) from Antalya, Turkey: polyphenol oxidase properties and anti-xanthine oxidase, anti-urease, and antioxidant activity

Investigation of a wild pear species (Pyrus elaeagnifoliasubsp.ElaeagnifoliaPallas) from Antalya, Turkey: polyphenol oxidase properties and anti-xanthine oxidase, anti-urease, and antioxidant activity

In vitro Antibacterial Activity of 7-Substituted-6-Fluoroquinolone and 7-Substituted-6,8-Difluoroquinolone Derivatives

Design, Synthesis, Antibacterial Evaluation and Docking Study of Novel 2‐Hydroxy‐3‐(nitroimidazolyl)‐propyl‐derived Quinolone

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