Muyocopronones A and B: azaphilones from the endophytic fungus Muyocopron laterale

• Ken-ichi Nakashima,
• Junko Tomida,
• Tomoe Tsuboi,
• Yoshiaki Kawamura and
• Makoto Inoue

Beilstein J. Org. Chem. 2020, 16, 2100–2107, doi:10.3762/bjoc.16.177

• Staphylococcus aureus (PAGU 273T), methicillin-resistant S. aureus (PAGU 841, MRSA), Staphylococcus epidermidis (PAGU 283T), Enterococcus faecalis (PAGU 102T), and vancomycin-resistant E. faecalis (PAGU 100, VRE). Piperacillin, vancomycin, and amikacin were used as positive controls. The isolated substances and

An overview of recent advances in duplex DNA recognition by small molecules

• Sayantan Bhaduri,
• Nihar Ranjan and
• Dev P. Arya

Beilstein J. Org. Chem. 2018, 14, 1051–1086, doi:10.3762/bjoc.14.93

Enduracididine, a rare amino acid component of peptide antibiotics: Natural products and synthesis

• Darcy J. Atkinson,
• Briar J. Naysmith,
• Daniel P. Furkert and
• Margaret A. Brimble

Beilstein J. Org. Chem. 2016, 12, 2325–2342, doi:10.3762/bjoc.12.226

• . Teixobactin (17) was isolated from the β-protobacterium, Eleftheria terrae that belongs to a new genus. Teixobactin (17) demonstrated potent activity against the resistant Gram-positive bacteria, MRSA and vancomycin-resistant Enterococci (VRE), as well as other bacterial species including, Mycobacterium

Muraymycin nucleoside-peptide antibiotics: uridine-derived natural products as lead structures for the development of novel antibacterial agents

• Daniel Wiegmann,
• Stefan Koppermann,
• Marius Wirth,
• Giuliana Niro,
• Kristin Leyerer and
• Christian Ducho

Beilstein J. Org. Chem. 2016, 12, 769–795, doi:10.3762/bjoc.12.77

• methicillin-resistant Staphylococcus aureus (MRSA) [18][19] and vancomycin-resistant Enterococcus (VRE) [20]. This development raises the demand for antibiotics exploiting yet unused modes of action. Potential targets within bacteria include peptidoglycan biosynthesis, protein biosynthesis, DNA and RNA

• , 92c) in order to investigate the role of the cyclic guanidine functionality (Figure 10) [77]. These compounds were all active against MRSA and VRE with varying MIC values (Table 2). The most active analogues of this series were 92a and 92b (Figure 10, highlighted in orange) with MIC values between 1

Effective in silico prediction of new oxazolidinone antibiotics: force field simulations of the antibiotic–ribosome complex supervised by experiment and electronic structure methods

• Jörg Grunenberg and
• Giuseppe Licari

Beilstein J. Org. Chem. 2016, 12, 415–428, doi:10.3762/bjoc.12.45

• portion displayed in blue [15]. While only the S-enantiomer seems to be potent, linezolid shows activity against a wide range of Gram-positive bacteria such as vancomycin-resistant Enterococcus (VRE), methicillin-resistant Staphylococcus aureus (MRSA) and penicillin-resistant Streptococcus pneumoniae

• aureus), VRE and Hi (Haemophilus influenzae) bacterial strains, it is currently undergoing clinical trials. An earlier docking study of 7 by Shaw et al. [47] postulated an increased potency mediated by additional interactions between the ribosomal active site and the pyridine and tetrazole rings from 7

The chemistry of isoindole natural products

• Klaus Speck and
• Thomas Magauer

Beilstein J. Org. Chem. 2013, 9, 2048–2078, doi:10.3762/bjoc.9.243

• natural product and synthetic precursor of 193 shows strong antibiotic activity against methicillin-resistant Staphylococcus aureus (MRSA, MIC = 84 nM) and vancomycin-resistant Enterococcus (VRE, MIC = 178 nM) [148]. The structural similarity between pestalachloride A (193) and pestalone (192), which both

• Enterococcus (VRE) [159]. Beyond that, the modest cytotoxic activity of 215 and 217 against human cancer cell lines makes them interesting lead components for drug discovery. The IC50 values of 215 for different leukemia cell lines range from 0.11–0.22 µM. For 217, an IC50 value of 0.32 µM against gastric

Synthesis and antibacterial activity of monocyclic 3-carboxamide tetramic acids

• Yong-Chul Jeong and
• Mark G. Moloney

Beilstein J. Org. Chem. 2013, 9, 1899–1906, doi:10.3762/bjoc.9.224

• susceptible Enterococcus faecalis (VSE, E1), vancomycin resistant E. faecium (VanA VRE, E2)), and 2 strains of Streptococcus pneumoniae, including multi-drug resistant strain (MDRSP, P9), as well as 3 species of Gram-negative bacteria, consisting of Pseudomonas aeruginosa and 2 strains of Haemophilus

• bacteria, although the activity depends on the substituent identities. Importantly, the variation of antibacterial activity for analogues 2 and 3 was less pronounced in the resistant strains MRSA, VRE and MDRSP (normally less than 8 times variation, with the exception of analogues 2e and 3b), while the

• activities of Novartis analogue 1c against MRSA [8], amoxicillin against MDRSP and ciprofloxacin against MRSA and VRE were significantly lower (more than 250 times compared with the activity against the most sensitive strain). Among the various substituent groups, N-alkyl phenyl derivatives 2a,b,h were

Binaphthyl-anchored antibacterial tripeptide derivatives with hydrophobic C-terminal amino acid variations

• John B. Bremner,
• Paul A. Keller,
• Stephen G. Pyne,
• Mark J. Robertson,
• K. Sakthivel,
• Kittiya Somphol,
• Dean Baylis,
• Jonathan A. Coates,
• John Deadman,
• Dharshini Jeevarajah and
• David I. Rhodes

Beilstein J. Org. Chem. 2012, 8, 1265–1270, doi:10.3762/bjoc.8.142

• and Enterococci (VRE, VSE), and against Staphylococcus epidermidis. Keywords: antibacterials; binaphthyls; cationic peptides; peptides; resistance; VISA; VRE; Introduction Among the most pressing challenges in current healthcare is the resistance of bacterial human pathogenic organisms to

• salts 2a–g were tested against the Gram-positive bacteria Staphylococcus aureus (ATCC 6538) and four clinical isolates of vancomycin-resistant (and sensitive) enterococci (VRE; Enterococcus faecium), and the results are shown in Table 1; some compounds were also tested against Staphylococcus epidermidis

• promising initial activity profile, the tripeptide derivative 2c was subjected to further evaluation (Table 2). It was tested against methicillin-sensitive (MSSA), methicillin-resistant (MRSA) and vancomycin-intermediate (VISA) S. aureus, S. epidermis and vancomycin-resistant (VRE) and vancomycin-sensitive