The global antibiotic research and development partnership (GARDP): researching and developing new antibiotics to meet global public health needs
On the road to structure-based development of anti-virulence therapeutics targeting the type III secretion system injectisome
Targeting the T3SS injectisome using the anti-virulence strategy offers an alternative to antibiotic therapeutic approaches when dealing with resistance.
Revitalizing antifolates through understanding mechanisms that govern susceptibility and resistance
Mechanisms of antifolate resistance in bacterial and mammalian cells.
Drug-resistance in Mycobacterium tuberculosis: where we stand
Inhibiting bacterial secretion systems in the fight against antibiotic resistance
The search for new ammunition to combat antibiotic resistance has uncovered diverse inhibitors of the bacterial type IV secretion system.
Gasdermin D (GSDMD) as a new target for the treatment of infection
Inhibition of pyroptosis through targeting the activation or pore-formation of GSDMD.
The calcium-dependent lipopeptide antibiotics: structure, mechanism, & medicinal chemistry
To push back the growing tide of antibacterial resistance the discovery and development of new antibiotics is a must.
Connecting iron acquisition and biofilm formation in the ESKAPE pathogens as a strategy for combatting antibiotic resistance
Biofilms are linked to resistance development in the ESKAPE pathogens. This perspective summarizes several strategies for affecting iron homeostasis that have been implicated in biofilm inhibition.
Methicillin-resistant Staphylococcus aureus (MRSA): antibiotic-resistance and the biofilm phenotype
Staphylococcus aureus (S. aureus) is an asymptomatic colonizer of 30% of all human beings. It is also the most dangerous of all Staphylococcal bacteria.
Novel zafirlukast derivatives exhibit selective antibacterial activity against Porphyromonas gingivalis
Eleven new zafirlukast derivatives selective and bactericidal against Porphyromonas gingivalis.
Fluoroquinolone-derived fluorescent probes for studies of bacterial penetration and efflux
Fluorescent probes derived from the fluoroquinolone antibiotic ciprofloxacin were synthesised using a Cu(I)-catalysed azide–alkyne cycloaddition (CuAAC) to link a ciprofloxacin azide derivative with alkyne-substituted green and blue fluorophores.
Anthranilic amide and imidazobenzothiadiazole compounds disrupt Mycobacterium tuberculosis membrane potential
Compounds 1 and 2 disrupt M. tuberculosis membrane potential and demonstrate bactericidal activity against non-replicating M. tuberculosis in pH 4.5 buffer.
Synthesis, ribosomal selectivity, and antibacterial activity of netilmicin 4′-derivatives
We describe the synthesis and evaluation of 4′-subsituted netilmicin derivatives by selective functionalization at the 4′-position of the endocyclic enolether function.
Biochemical and microbiological evaluation of N-aryl urea derivatives against mycobacteria and mycobacterial hydrolases
N-Aryl urea derivatives were synthesized and some showed activity against mycobacterial hydrolases while others showed antimicrobial activity against mycobacterial species.
Synthetic studies on the reverse antibiotic natural products, the nybomycins
We report a new scalable and robust synthetic route to the nybomycin natural products and the activity of novel analogues of this family.
Iridium piano stool complexes with activity against S. aureus and MRSA: it is past time to truly think outside of the box
Iridium based antimicrobial agents have shown efficacy against S. aureus, including MRSA, and appear to be safe in mice.
Eradicating uropathogenic Escherichia coli biofilms with a ciprofloxacin–dinitroxide conjugate
Biofilm-related UTIs are problematic infectious diseases worldwide; here we have developed a novel ciprofloxacin–dinitroxide conjugate with potent UPEC biofilm-eradication activity.
Rapid kill assessment of an N-arylated NH125 analogue against drug-resistant microorganisms
N-Arylated NH125 analogue 1 rapidly eradicates a diverse panel of drug-resistant bacteria and fungi (≥99.9% kill in 1 to 10 minutes).
Synthesis of saccharocin from apramycin and evaluation of its ribosomal selectivity
We describe a facile synthesis of saccharocin from apramycin by regioselective tetra-azidation and stereospecific oxidative deamination of the amino group.
Polybasic peptide–levofloxacin conjugates potentiate fluoroquinolones and other classes of antibiotics against multidrug-resistant Gram-negative bacteria
To address the rising threat of multidrug-resistant (MDR) bacteria, new therapeutic strategies must be developed.
Using 2-aminobenzimidazole derivatives to inhibit Mycobacterium smegmatis biofilm formation
Biofilm formation by mycobacteria can lead to enhanced antibiotic tolerance.
‘Second-generation’ 1,2,3-triazole-based inhibitors of Porphyromonas gingivalis adherence to oral streptococci and biofilm formation
This study details the design, synthesis and bioassay of ‘click’ peptidomimetic compounds which inhibit the adherence of P. gingivalis to S. gordonii, a primary step toward pathogenic colonization of the subgingival pocket.
Structure–activity relationship of the cinnamamide family of antibiotic potentiators for methicillin-resistant Staphylococcus aureus (MRSA)
MIC of oxacillin against S. aureus (MRSA252 strain) reduced from 256 μg mL−1 to 2 μg mL−1.