Antibacterial activity of head-to-head bis-benzimidazoles

Synthesis and structure–activity relationship of amidine derivatives of 3,4-ethylenedioxythiophene as novel antibacterial agents

“…Several bis-benzimidazoles have shown significant antibacterial activities against drug-resistant bacteria (methicillin-resistant Staphylococcus aureus -MRSA and methicillin resistant S. epidermidis -MRSE and vancomycin resistant enterococci -VRE strains) [19,37]. In addition, diamidine derivatives of bis-indoles, as structural analogues of benzimidazoles, were shown to exhibit in vitro activity against a broad spectrum of Gramnegative and Gram-positive pathogens such as S. aureus (including MRSA) and E. faecalis (including VRE) which additionally supports the use of mono-and bis-benzimidazole units in 3,4-ethylenedioxythiophene series [21,24].…”

The discovery of a novel antibiotic for the treatment of Clostridium difficile infections: a story of an effective academic–industrial partnership

“…A graduate student on the Royal Pharmaceutical Society award, Joao Moreira, profiled 21 symmetric and asymmetric BBZs against a comprehensive panel of Gram-positive clinical isolates, including ten from the initial series synthesised by John Mann and co-workers. This in-depth study 23 confirmed the lack of activity against a wide range of Gram-negative pathogens but established that three compounds in particular possessed potent anti-staphylococcal activity against four methicillin-susceptible S. aureus and 61 MRSA strains from Peter Taylor's extensive international collection of clinical isolates, with clinically attractive MIC 90 values (MIC required to inhibit 90% of the isolates) in the sub-μg ml –1 range. Similar potent effects were recorded against vancomycin intermediate-susceptible S. aureus (VISA; clinically troublesome MRSA partially resistant to the drug of last resort), Streptococcus pyogenes , Streptococcus agalactiae and β-haemolytoc streptococci.…”

Antimicrobial potential of 1H-benzo[d]imidazole scaffold: a review

“…Compounds 26c and 26d exhibited significant activity against M. tuberculosis H37Rv with MIC value of 2 mg/L and 1 mg/L, respectively (Fig. 6) [34].…”