Fluoroquinolones structural and medicinal developments (2013–2018): Where are we now?

Suaifan, Ghadeer A. R. Y.; Mohammed, Aya A.M.

doi:10.1016/j.bmc.2019.05.038

Cited by 64 publications

(40 citation statements)

References 87 publications

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“…Fluoroquinolones (FQs) represent one of the most commonly used antibiotics to treat human and veterinary infections due to their excellent bioavailability, good tissue penetration, relatively low toxicity, and broad-spectrum activity [13][14][15] . Numerous FQ derivatives have been synthesized by modifying the chemical structure of the 1,8 naphthyridine core in order to increase their antibacterial efficiency and improve their pharmacokinetics [16][17][18][19][20] . These modifications have led to the synthesis of norfloxacin and ciprofloxacin, two antibiotics with increased activity against Gram-negative bacteria, which are still marketed 13 .…”

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The challenge of intracellular antibiotic accumulation, a function of fluoroquinolone influx versus bacterial efflux

et al. 2020

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With the spreading of antibiotic resistance, the translocation of antibiotics through bacterial envelopes is crucial for their antibacterial activity. In Gram-negative bacteria, the interplay between membrane permeability and drug efflux pumps must be investigated as a whole. Here, we quantified the intracellular accumulation of a series of fluoroquinolones in population and in individual cells of Escherichia coli according to the expression of the AcrB efflux transporter. Computational results supported the accumulation levels measured experimentally and highlighted how fluoroquinolones side chains interact with specific residues of the distal pocket of the AcrB tight monomer during recognition and binding steps.

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The challenge of intracellular antibiotic accumulation, a function of fluoroquinolone influx versus bacterial efflux

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“…Antimicrobial properties of halogens are a well described mechanism that has been used in the design of most common antimicrobial agents, such chloramphenicol or vancomycin (which contain chlorine), or fluoroquinolones (which contains fluorine) [ 54 ]. Polymers containing halogens combine the antimicrobial properties of both structures, thus leading to an improvement of therapeutic efficacy.…”

Section: Polymers As a New Generation Of Antibacterial Agentsmentioning

confidence: 99%

State-of-the-art polymeric nanoparticles as promising therapeutic tools against human bacterial infections

et al. 2020

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Infectious diseases kill over 17 million people a year, among which bacterial infections stand out. From all the bacterial infections, tuberculosis, diarrhoea, meningitis, pneumonia, sexual transmission diseases and nosocomial infections are the most severe bacterial infections, which affect millions of people worldwide. Moreover, the indiscriminate use of antibiotic drugs in the last decades has triggered an increasing multiple resistance towards these drugs, which represent a serious global socioeconomic and public health risk. It is estimated that 33,000 and 35,000 people die yearly in Europe and the United States, respectively, as a direct result of antimicrobial resistance. For all these reasons, there is an emerging need to find novel alternatives to overcome these issues and reduced the morbidity and mortality associated to bacterial infectious diseases. In that sense, nanotechnological approaches, especially smart polymeric nanoparticles, has wrought a revolution in this field, providing an innovative therapeutic alternative able to improve the limitations encountered in available treatments and capable to be effective by theirselves. In this review, we examine the current status of most dangerous human infections, together with an in-depth discussion of the role of nanomedicine to overcome the current disadvantages, and specifically the most recent and innovative studies involving polymeric nanoparticles against most common bacterial infections of the human body.

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“…In recent years, several fluoroquinolone derivatives were synthesized and approved by FDA as a broad spectrum, antibacterial agents used in the treatment of respiratory and urinary tract infections [ 1 , 2 ]. These drugs are effective in the treatment of the hospital-acquired infections in which resistance to older antibacterial classes is suspected [ 3 ].…”

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Ciprofloxacin and moxifloxacin could interact with SARS-CoV-2 protease: preliminary in silico analysis

et al. 2020

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Background A large body of research has focused on fluoroquinolones. It was shown that this class of synthetic antibiotics could possess antiviral activity as a broad range of anti-infective activities. Based on these findings, we have undertaken in silico molecular docking study to demonstrate, for the first time, the principle for the potential evidence pointing ciprofloxacin and moxifloxacin ability to interact with COVID-19 Main Protease. Methods In silico molecular docking and molecular dynamics techniques were applied to assess the potential for ciprofloxacin and moxifloxacin interaction with COVID-19 Main Protease (Mpro). Chloroquine and nelfinavir were used as positive controls. Results We revealed that the tested antibiotics exert strong capacity for binding to COVID-19 Main Protease (Mpro). According to the results obtained from the GOLD docking program, ciprofloxacin and moxifloxacin bind to the protein active site more strongly than the native ligand. When comparing with positive controls, a detailed analysis of the ligand–protein interactions shows that the tested fluoroquinolones exert a greater number of protein interactions than chloroquine and nelfinavir. Moreover, lower binding energy values obtained from KDEEP program were stated when compared to nelfinavir. Conclusions Here, we have demonstrated for the first time that ciprofloxacin and moxifloxacin may interact with COVID-19 Main Protease (Mpro).

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Fluoroquinolones structural and medicinal developments (2013–2018): Where are we now?

Cited by 64 publications

References 87 publications

The challenge of intracellular antibiotic accumulation, a function of fluoroquinolone influx versus bacterial efflux

The challenge of intracellular antibiotic accumulation, a function of fluoroquinolone influx versus bacterial efflux

State-of-the-art polymeric nanoparticles as promising therapeutic tools against human bacterial infections

Ciprofloxacin and moxifloxacin could interact with SARS-CoV-2 protease: preliminary in silico analysis

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