Specialty Grand Challenge In Pediatric Infectious Diseases

Lepage, Philippe

doi:10.3389/fped.2017.00185

Cited by 5 publications

(3 citation statements)

References 57 publications

(69 reference statements)

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“…Today, MDR has attracted increasing attention because of the recent statistics reported by the World Health Organization (WHO). According to the WHO, around 50,000 patients die from infectious diseases every day worldwide [6]. Oxazolidinones are a new class of antimicrobial agents that have a unique structure and show good activity against different pathogenic bacteria, including methicillin-and vancomycin-resistant staphylococci, vancomycin-resistant enterococci, penicillin-resistant pneumococci, and anaerobes [7].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Antibacterial Evaluation, and Computational Studies of a Diverse Set of Linezolid Conjugates

et al. 2022

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The development of new antibiotics to treat multidrug-resistant (MDR) bacteria or possess broad-spectrum activity is one of the challenging tasks. Unfortunately, there are not many new antibiotics in clinical trials. So, the molecular hybridization approach could be an effective strategy to develop potential drug candidates using the known scaffolds. We synthesized a total of 31 diverse linezolid conjugates 3, 5, 7, 9, 11, 13, and 15 using our established benzotriazole chemistry with good yield and purity. Some of the synthesized conjugates exhibited promising antibacterial properties against different strains of bacteria. Among all the synthesized compounds, 5d is the most promising antibacterial agent with MIC 4.5 µM against S. aureus and 2.25 µM against B. subtilis. Using our experimental data pool, we developed a robust QSAR (R2 = 0.926, 0.935; R2cvOO = 0.898, 0.915; R2cvMO = 0.903, 0.916 for the S. aureus and B. subtilis models, respectively) and 3D-pharmacophore models. We have also determined the drug-like properties of the synthesized conjugates using computational tools. Our findings provide valuable insight into the possible linezolid-based antibiotic drug candidates.

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Section: Introductionmentioning

confidence: 99%

Synthesis, Antibacterial Evaluation, and Computational Studies of a Diverse Set of Linezolid Conjugates

et al. 2022

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“…This makes both Gram-positive and Gram-negative bacteria appear severely resistant. , Horizontal transfer by bacteria to obtain exogenous drug-resistance genes also accelerates the production of drug-resistant strains . According to statistics from the World Health Organization (WHO), ∼50 000 patients die from infectious diseases every day worldwide, seriously threatening human health and social development; as a result, drug-resistant strains have attracted increasing attention . Of these, the trouble of multi-drug-resistant bacteria is especially prominent.…”

Section: Introductionmentioning

confidence: 99%

“…6 According to statistics from the World Health Organization (WHO), ∼50 000 patients die from infectious diseases every day worldwide, seriously threatening human health and social development; as a result, drugresistant strains have attracted increasing attention. 7 Of these, the trouble of multi-drug-resistant bacteria is especially prominent. In particular, methicillin-resistant Staphylococcus aureus (MRSA), methicillin-resistant Staphylococcus epidermidis (MRSE), penicillin-resistant multi-drug-resistant tuberculosis (MDR-TB), vancomycin-resistant Enterococcus (VRE), Streptococcus pneumoniae (PRSP), and other Gram-positive bacteria are the most prevalent, and they make clinical treatment very difficult.…”

Section: Introductionmentioning

confidence: 99%

Current Landscape and Future Perspective of Oxazolidinone Scaffolds Containing Antibacterial Drugs

et al. 2021

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The widespread use of antibiotics has made the problem of bacterial resistance increasingly serious, and the study of new drug-resistant bacteria has become the main direction of antibacterial drug research. Among antibiotics, the fully synthetic oxazolidinone antibacterial drugs linezolid and tedizolid have been successfully marketed and have achieved good clinical treatment effects. Oxazolidinone antibacterial drugs have good pharmacokinetic and pharmacodynamic characteristics and unique antibacterial mechanisms, and resistant bacteria are sensitive to them. This Perspective focuses on reviewing oxazolidinones based on the structural modification of linezolid and new potential oxazolidinone drugs in the past 10 years, mainly describing their structure, antibacterial activity, safety, druggability, and so on, and discusses their structure−activity relationships, providing insight into the reasonable design of safer and more potent oxazolidinone antibacterial drugs.

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