Themed collection Antimicrobial Resistance

23 items
Editorial

Introduction to the themed collection on antimicrobial resistance

Guest editors Jayanta Haldar, Sylvie Garneau-Tsodikova and Micha Fridman introduce the RSC Medicinal Chemistry themed collection on ‘Antibiotic microbial resistance’.

Graphical abstract: Introduction to the themed collection on antimicrobial resistance
From the themed collection: Antimicrobial Resistance
Review Article

Chemical genetic approaches for the discovery of bacterial cell wall inhibitors

High-throughput chemical genetic screening strategies for bacterial cell envelope inhibitors.

Graphical abstract: Chemical genetic approaches for the discovery of bacterial cell wall inhibitors
From the themed collection: Antimicrobial Resistance
Review Article

Restoring susceptibility to aminoglycosides: identifying small molecule inhibitors of enzymatic inactivation

Growing resistance to antimicrobial medicines is a critical health problem that must be urgently addressed.

Graphical abstract: Restoring susceptibility to aminoglycosides: identifying small molecule inhibitors of enzymatic inactivation
From the themed collection: Antimicrobial Resistance
Review Article

Recent developments in membrane targeting antifungal agents to mitigate antifungal resistance

Fungal infections cause severe and life-threatening complications especially in immunocompromised individuals.

Graphical abstract: Recent developments in membrane targeting antifungal agents to mitigate antifungal resistance
From the themed collection: Antimicrobial Resistance
Review Article

Dual functional therapeutics: mitigating bacterial infection and associated inflammation

Dual-functional therapeutics with the ability to tackle both bacterial infection and associated hyper-inflammation hold great promise for mitigating complicated infections and sepsis.

Graphical abstract: Dual functional therapeutics: mitigating bacterial infection and associated inflammation
From the themed collection: Antimicrobial Resistance
Review Article

Siderophore conjugates to combat antibiotic-resistant bacteria

Antimicrobial resistance (AMR) is a global threat to society due to the increasing emergence of multi-drug resistant bacteria that are not susceptible to our last line of defence antibiotics: new approaches are needed to fight back.

Graphical abstract: Siderophore conjugates to combat antibiotic-resistant bacteria
From the themed collection: Antimicrobial Resistance
Review Article

Ribosome-targeting antibiotics and resistance via ribosomal RNA methylation

The rise of multidrug-resistant bacterial infections is a cause of global concern.

Graphical abstract: Ribosome-targeting antibiotics and resistance via ribosomal RNA methylation
From the themed collection: Antimicrobial Resistance
Review Article

The role of adjuvants in overcoming antibacterial resistance due to enzymatic drug modification

Enzymatic drug deactivation is an important contributor to bacterial resistance. Adjuvants which inhibit the β-lactamases help maintain the efficacy of the β-lactams, demonstrating the potential for this strategy for other antibacterial classes.

Graphical abstract: The role of adjuvants in overcoming antibacterial resistance due to enzymatic drug modification
From the themed collection: Antimicrobial Resistance
Open Access Research Article

Inhibition of DXR in the MEP pathway with lipophilic N-alkoxyaryl FR900098 analogs

Isoprene biosynthesis is a point of vulnerability for many pathogens. Building on prior work, we report a novel set of potent compounds that display selectivity for P. falciparum over M. tuberculosis, and act on-target intracellularly.

Graphical abstract: Inhibition of DXR in the MEP pathway with lipophilic N-alkoxyaryl FR900098 analogs
From the themed collection: Antimicrobial Resistance
Research Article

Discovery of benzoxazole–thiazolidinone hybrids as promising antibacterial agents against Staphylococcus aureus and Enterococcus species

Increase in activity of B–T hybrids with halo-salicyl group on thiazolidinone against S. aureus ATCC 29213.

Graphical abstract: Discovery of benzoxazole–thiazolidinone hybrids as promising antibacterial agents against Staphylococcus aureus and Enterococcus species
From the themed collection: Antimicrobial Resistance
Research Article

Enhancing allosteric inhibition of dihydrodipicolinate synthase through the design and synthesis of novel dimeric compounds

The synthesis of the first low micromolar dimeric inhibitor of E. coli DHDPS is reported.

Graphical abstract: Enhancing allosteric inhibition of dihydrodipicolinate synthase through the design and synthesis of novel dimeric compounds
From the themed collection: Antimicrobial Resistance
Research Article

Design, synthesis and evaluation of halogenated phenazine antibacterial prodrugs targeting nitroreductase enzymes for activation

In this study, we have designed, synthesized, and evaluated new halogenated phenazine prodrugs that could lead to breakthroughs in the treatment of antibiotic-resistant bacterial infections.

Graphical abstract: Design, synthesis and evaluation of halogenated phenazine antibacterial prodrugs targeting nitroreductase enzymes for activation
From the themed collection: Antimicrobial Resistance
Research Article

Discovery and development of novel substituted monohydrazides as potent antifungal agents

Novel substituted monohydrazides synthesized for this study displayed broad-spectrum activity against various fungal strains, including a panel of clinically relevant Candida auris strains.

Graphical abstract: Discovery and development of novel substituted monohydrazides as potent antifungal agents
From the themed collection: Antimicrobial Resistance
Research Article

Detection of intact vancomycin–arginine as the active antibacterial conjugate in E. coli by whole-cell solid-state NMR

Vancomycin–arginine (V–R) is effective against antibiotic-resistant Gram-negative pathogens. We designed a whole-cell solid-state NMR approach and detected intact V–R in E. coli, indicating no hydrolysis or liberation of the conjugated arginine.

Graphical abstract: Detection of intact vancomycin–arginine as the active antibacterial conjugate in E. coli by whole-cell solid-state NMR
From the themed collection: Antimicrobial Resistance
Research Article

Synthesis of tryptanthrin appended dispiropyrrolidine oxindoles and their antibacterial evaluation

The synthesis of sixteen tryptanthrin appended dispiropyrrolidine oxindoles, employing [3 + 2] cycloaddition of tryptanthrin-derived azomethine ylides with isatilidenes, and their detailed antibacterial evaluation is described.

Graphical abstract: Synthesis of tryptanthrin appended dispiropyrrolidine oxindoles and their antibacterial evaluation
From the themed collection: Antimicrobial Resistance
Research Article

Identification and analysis of small molecule inhibitors of FosB from Staphylococcus aureus

High-throughput virtual screening has identified several new inhibitors of FosB from methicillin-resistant Staphylococcus aureus.

Graphical abstract: Identification and analysis of small molecule inhibitors of FosB from Staphylococcus aureus
From the themed collection: Antimicrobial Resistance
Research Article

Mycobacterium tuberculosis CitA activity is modulated by cysteine oxidation and pyruvate binding

The M. tuberculosis citrate synthase regulatory domain binds pyruvate to affect enzyme activity while cysteine oxidation in the same domain eliminates enzyme activity. This affords regulatory control at the protein level of entry to the TCA cycle.

Graphical abstract: Mycobacterium tuberculosis CitA activity is modulated by cysteine oxidation and pyruvate binding
From the themed collection: Antimicrobial Resistance
Research Article

Semisynthetic blasticidin S ester derivatives show enhanced antibiotic activity

A potential rich source of new antimicrobials is undeveloped natural product cytotoxins. We used semisynthesis to derivatize the neglected antibiotic blasticidin S, creating ester derivatives with enhanced selectivity for bacteria.

Graphical abstract: Semisynthetic blasticidin S ester derivatives show enhanced antibiotic activity
From the themed collection: Antimicrobial Resistance
Research Article

Inhibition and eradication of Pseudomonas aeruginosa biofilms by secondary metabolites of Nocardiopsis lucentensis EMB25

Promising activity of secondary metabolites extracted from a rare actinobacteria, Nocardiopsis lucentensis EMB25 against biofilm of Pseudomonas aeruginosa.

Graphical abstract: Inhibition and eradication of Pseudomonas aeruginosa biofilms by secondary metabolites of Nocardiopsis lucentensis EMB25
From the themed collection: Antimicrobial Resistance
Research Article

Dimeric polyphenols to pave the way for new antimalarial drugs

A polyphenolic scaffold to develop novel orally active antimalarials against resistant Plasmodium falciparum.

Graphical abstract: Dimeric polyphenols to pave the way for new antimalarial drugs
From the themed collection: Antimicrobial Resistance
Research Article

The Mycobacterium tuberculosis mycothiol S-transferase is divalent metal-dependent for mycothiol binding and transfer

Mycothiol S-transferase (MST) (encoded by the rv0443 gene) was previously identified as the enzyme responsible for the transfer of mycothiol (MSH) to xenobiotic acceptors in Mycobacterium tuberculosis (M.tb) during xenobiotic stress.

Graphical abstract: The Mycobacterium tuberculosis mycothiol S-transferase is divalent metal-dependent for mycothiol binding and transfer
From the themed collection: Antimicrobial Resistance
Research Article

Expanding the structure–activity relationships of alkynyl diphenylurea scaffold as promising antibacterial agents

With the continuous and alarming threat of exhausting the current antimicrobial arsenals, efforts are urgently needed to develop new effective ones.

Graphical abstract: Expanding the structure–activity relationships of alkynyl diphenylurea scaffold as promising antibacterial agents
From the themed collection: Antimicrobial Resistance
Open Access Research Article

Synthesis and structure–activity relationship studies of N-terminal analogues of the lipopeptide antibiotics brevicidine and laterocidine

SAR studies on brevicidine and laterocidine yield new analogues with strong activity against multidrug-resistant Gram-negative bacteria.

Graphical abstract: Synthesis and structure–activity relationship studies of N-terminal analogues of the lipopeptide antibiotics brevicidine and laterocidine
From the themed collection: Antimicrobial Resistance
23 items

About this collection

This themed collection, guest edited by Professor Micha Fridman (Tel Aviv University, Israel), Professor Sylvie Garneau-Tsodikova (University of Kentucky, USA) and Professor Jayanta Haldar (Jawaharlal Nehru Centre for Advanced Scientific Research, India), highlights the latest medicinal chemistry advances in tackling drug resistance. This collection covers various areas related to antimicrobial (fungi, bacteria, and viruses) drug discovery and development, as well as research towards understanding the mechanisms of resistance.

New articles will be added to the collection upon publication. Please return to this page frequently to see the collection grow.

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