Themed collection Antimicrobial Resistance

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

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

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

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

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

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.

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

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.

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.

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

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

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.

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

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.

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.

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

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.

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.

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

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

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.

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

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