Synthesis, ribosomal selectivity, and antibacterial activity of netilmicin 4′-derivatives

Sonousi, Amr; Shcherbakov, Dimitri; Vasella, Andrea; Böttger, Erik C.; Crich, David

doi:10.1039/c9md00153k

Cited by 2 publications

(1 citation statement)

References 19 publications

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“…Mycobacterium tuberculosis spreads to multiple parts of the body and triggers infection of the respiratory system, followed by pulmonary infection, ultimately leading to TB. Ordinarily, malnourished and immuno-compromised elderly people are highly prone to infection with Mycobacterium tuberculosis [13][14][15].…”

Section: Discussionmentioning

confidence: 99%

Effectiveness and safety of co-administration of moxifloxacin with netilmicin in drug-resistant tuberculosis patients, and its impact on inflammatory factors and immune function

Wang¹,

Zhang²,

Chen³

et al. 2022

Trop. J. Pharm Res

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Purpose: To study the effectiveness and safety of co-administration of moxifloxacin with netilmicin in drug-resistant tuberculosis (TB) patients, and its impact on levels of inflammatory factors and immune function. Methods: We enrolled 100 patients with drug-resistant TB admitted to People’s Hospital of Rizhao between May 2017 and October 2019. The patients were randomly allocated to control group and study group, with 50 patients per group. The control group received moxifloxacin at a dose of 0.2 g t.i.d. for 6 months and the study group received netilmicin at a dose of 0.1 g t.i.d. plus. The response, incidence of adverse reactions, expression levels of inflammatory factors, immune function, and sputum-negative status after 2, 4 and 6 months of TB treatment were compared. Results: The study group showed markedly higher response than the control group (p < 0.05). Moreover, there were lower incidence of adverse effects in the study group than in the control group (p < 0.05). The expression levels of inflammatory factors were significantly lower in the study group, while the concentrations of CD3+, CD4+, and CD8+ were markedly higher (p < 0.05). After 2, 4 and 6 months of TB treatment, cases of sputum-negative conversion were significantly higher in the study group than in the control group (p < 0.05). Conclusion: Co-administration of moxifloxacin with netilmicin produces much higher effectiveness and safety than moxifloxacin monotherapy, decreases inflammatory factor levels and improves immune function in patients with drug-resistant TB.

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Section: Discussionmentioning

confidence: 99%

Effectiveness and safety of co-administration of moxifloxacin with netilmicin in drug-resistant tuberculosis patients, and its impact on inflammatory factors and immune function

Wang¹,

Zhang²,

Chen³

et al. 2022

Trop. J. Pharm Res

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Design, Synthesis and Activity Evaluation Against Drug‐Resistant Bacteria of 6’‐Amidine Modified Aminoglycoside Derivatives

Xu,

Zhang,

et al. 2024

ChemistrySelect

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The issue of bacterial resistance has become a matter of significant concern globally, prompting extensive research into the development and clinical application of aminoglycoside antibiotics (AGAs) as a crucial antibacterial therapy. One of the primary mechanisms contributing to aminoglycoside antibiotic resistance is the action of aminoglycoside modifying enzymes (AMEs), which modify aminoglycoside antibiotics and consequently confer drug resistance. Chemical modification of the AME action site can eliminate functional groups vulnerable to AMEs, thus improving drug resistance. This study involves the introduction of α‐hydroxy‐γ‐aminobutyric acid and amidine to the 1 and 6′ positions of sisomicin, respectively, to produce a range of 6′‐amidine modified sisomicin derivatives of AGAs. The research evaluates the antibacterial activity, absorption, distribution, metabolism, and excretion (ADME) properties, pharmacokinetic properties, cytotoxicity, nephrotoxicity, and drug resistance of AGAs. The outcomes of this study are significant in terms of enriching the structural understanding of aminoglycosides, providing insight into their structure–activity relationship, and producing new AGAs with high antibacterial activity, low ototoxicity, and nephrotoxicity.

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Synthesis, ribosomal selectivity, and antibacterial activity of netilmicin 4′-derivatives

Abstract: We describe the synthesis and evaluation of 4′-subsituted netilmicin derivatives by selective functionalization at the 4′-position of the endocyclic enolether function.

Cited by 2 publications

References 19 publications

Effectiveness and safety of co-administration of moxifloxacin with netilmicin in drug-resistant tuberculosis patients, and its impact on inflammatory factors and immune function

Effectiveness and safety of co-administration of moxifloxacin with netilmicin in drug-resistant tuberculosis patients, and its impact on inflammatory factors and immune function

Design, Synthesis and Activity Evaluation Against Drug‐Resistant Bacteria of 6’‐Amidine Modified Aminoglycoside Derivatives

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