Structure-Activity Relationships and Mechanism of Action of Macrolides Derived from Erythromycin as Antibacterial Agents

Liang, Jianhua; Han, Xu

doi:10.2174/15680266113136660223

Cited by 44 publications

(14 citation statements)

References 200 publications

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“…Erythromycin is a bacteriostatic antibiotic, which means that it prevents the further growth of bacteria rather than directly destroying it. This action occurs by inhibiting protein synthesis [65]. Table S4 summarizes the observations made for some previously reported GO NS (variations of ZOI from 7 to 12 mm).…”

Section: Antibacterial Activity Studiesmentioning

confidence: 94%

Chloramine-T/N-Bromosuccinimide/FeCl3/KIO3 Decorated Graphene Oxide Nanosheets and Their Antibacterial Activity

Hashmi¹,

Singh²,

Jain³

et al. 2020

Nanomaterials

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In this work, we report the synthesis of graphene oxide nanosheets (GO NS) using four different oxidants, namely, chloramine-T (CAT), FeCl 3 , N-bromosuccinimide (NBS), and KIO 3 . Fourier transform infrared spectroscopy (FTIR) was used to characterize the functional groups present in the synthesized GO. The microstructure analysis was performed using X-ray diffraction (XRD) and scanning electron microscopy (SEM) to investigate the morphology of GO. High-resolution transmission electron microscopy (HRTEM) studies demonstrated the nanostructure and crystalline phases of GO. The antibacterial activity of the prepared GO NS was investigated against pure cultures of Pseudomonas pneumonia and Staphylococcus aureus. The synthesized GO NS with CAT-GO (C-GO) exhibited very good antibacterial activity towards pathogens.

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Section: Antibacterial Activity Studiesmentioning

confidence: 94%

Chloramine-T/N-Bromosuccinimide/FeCl3/KIO3 Decorated Graphene Oxide Nanosheets and Their Antibacterial Activity

Hashmi¹,

Singh²,

Jain³

et al. 2020

Nanomaterials

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“…Lastly, modifications also included replacement of desosamine with different sugars (Liang et al ., ; Romero et al ., ; Chen et al ., ). A detailed review covering all the chemical efforts to improve the ketolide activity is presented in the review of Liang and Han (). The only third‐generation macrolide in the market today is telithromycin (Figure ), commercialized as Ketek by Aventis, a 14‐membered ‘ketolide’ that was derived from clarithromycin using eight chemical steps (Denis et al ., ).…”

Section: Antimicrobial Activity and Chemical Derivatizationmentioning

confidence: 99%

“…Unlike macrolides, which are considered as time‐dependent bacteriocides, ketolides show concentration‐dependent killing (Zhanel and Hoban, ; Woosley et al ., ). In addition to the three ketolides mentioned above, other ketolide compounds have been developed, although none of them have so far attracted much attention (Fu et al ., ; Karahalios et al ., ; Kouvela et al ., ; Liang and Han, ; Ruan et al ., ; Krokidis et al ., ).…”

Section: Antimicrobial Activity and Chemical Derivatizationmentioning

confidence: 99%

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The macrolide antibiotic renaissance

Dinos

2017

British J Pharmacology

326

221

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Macrolides represent a large family of protein synthesis inhibitors of great clinical interest due to their applicability to human medicine. Macrolides are composed of a macrocyclic lactone of different ring sizes, to which one or more deoxy-sugar or amino sugar residues are attached. Macrolides act as antibiotics by binding to bacterial 50S ribosomal subunit and interfering with protein synthesis. The high affinity of macrolides for bacterial ribosomes, together with the highly conserved structure of ribosomes across virtually all of the bacterial species, is consistent with their broad-spectrum activity. Since the discovery of the progenitor macrolide, erythromycin, in 1950, many derivatives have been synthesised, leading to compounds with better bioavailability and acid stability and improved pharmacokinetics. These efforts led to the second generation of macrolides, including well-known members such as azithromycin and clarithromycin. Subsequently, in order to address increasing antibiotic resistance, a third generation of macrolides displaying improved activity against many macrolide resistant strains was developed. However, these improvements were accompanied with serious side effects, leading to disappointment and causing many researchers to stop working on macrolide derivatives, assuming that this procedure had reached the end. In contrast, a recent published breakthrough introduced a new chemical platform for synthesis and discovery of a wide range of diverse macrolide antibiotics. This chemical synthesis revolution, in combination with reduction in the side effects, namely, 'Ketek effects', has led to a macrolide renaissance, increasing the hope for novel and safe therapeutic agents to combat serious human infectious diseases.

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“…Macrolides inhibit bacteria protein biosynthesis by preventing peptidyltransferase location and/or inhibiting ribosomal translation (Tenson et al, 2003 ; Liang and Han, 2013 ). Macrolides were the first choice for treatment infections caused by Gram-positive bacteria in animal and campylobacterosis in human.…”

Section: Macrolides and Resistance In Campylobactermentioning

confidence: 99%

The Risk of Some Veterinary Antimicrobial Agents on Public Health Associated with Antimicrobial Resistance and their Molecular Basis

et al. 2016

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The risk of antimicrobial agents used in food-producing animals on public health associated with antimicrobial resistance continues to be a current topic of discussion as related to animal and human public health. In the present review, resistance monitoring data, and risk assessment results of some important antimicrobial agents were cited to elucidate the possible association of antimicrobial use in food animals and antimicrobial resistance in humans. From the selected examples, it was apparent from reviewing the published scientific literature that the ban on use of some antimicrobial agents (e.g., avoparcin, fluoroquinolone, tetracyclines) did not change drug resistance patterns and did not mitigate the intended goal of minimizing antimicrobial resistance. The use of some antimicrobial agents (e.g., virginiamycin, macrolides, and cephalosporins) in food animals may have an impact on the antimicrobial resistance in humans, but it was largely depended on the pattern of drug usage in different geographical regions. The epidemiological characteristics of resistant bacteria were closely related to molecular mechanisms involved in the development, fitness, and transmission of antimicrobial resistance.

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Structure-Activity Relationships and Mechanism of Action of Macrolides Derived from Erythromycin as Antibacterial Agents

Cited by 44 publications

References 200 publications

Chloramine-T/N-Bromosuccinimide/FeCl3/KIO3 Decorated Graphene Oxide Nanosheets and Their Antibacterial Activity

Chloramine-T/N-Bromosuccinimide/FeCl3/KIO3 Decorated Graphene Oxide Nanosheets and Their Antibacterial Activity

The macrolide antibiotic renaissance

The Risk of Some Veterinary Antimicrobial Agents on Public Health Associated with Antimicrobial Resistance and their Molecular Basis

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