Modulating the activity of short arginine-tryptophan containing antibacterial peptides with N-terminal metallocenoyl groups

• H. Bauke Albada,
• Alina-Iulia Chiriac,
• Michaela Wenzel,
• Maya Penkova,
• Julia E. Bandow,
• Hans-Georg Sahl and
• Nils Metzler-Nolte

Beilstein J. Org. Chem. 2012, 8, 1753–1764, doi:10.3762/bjoc.8.200

• running dry [1]. For example, the number of methicillin-resistant Staphylococcus aureus (MRSA) infections in hospitals are still very high and new infectious agents like Acinetobacter baumannii are on the rise, both leading to increased numbers of mortality. In view of this, the discovery of host-defense

• , replacement of the ruthenium atom with iron, going from RcCO to FcCO, results in a 4-fold and 8-fold drop in activity against B. subtilis and S. aureus (MRSA), respectively, even though their hydrophobicity is very similar. Since Rc is slightly larger than Fc – i.e., metal–carbon bonds in the first are 221

• in Table 2) The minimal inhibitory concentrations (MIC) were tested against Escherichia coli DSM 30083, Acinetobacter baumannii DSM 30007, Pseudomonas aeruginosa DSM 50071, Bacillus subtilis DSM 402, Staphylococcus aureus DSM 20231 (type strain), and Staphylococcus aureus ATCC 43300 (MRSA) in a

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

• 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

• MSSA, MRSA, VISA and VRE organisms. Our results confirmed the positive contribution to good Gram-positive antibacterial activity, engendered by filling of a hydrophobic area close to the C-terminus of these acyclic tripeptide derivatives. Experimental General notes were those detailed previously in the

• concentration of 128 µg/mL, in a 96-well plate. Plates were incubated overnight at 37 °C and the MIC was recorded as the highest concentration at which bacterial growth was observed. Compound 2c (Table 2) was tested at JMI Laboratories through Ordway Research Institute (USA) on Staphylococcus aureus (MSSA; MRSA

Synthesis, reactivity and biological activity of 5-alkoxymethyluracil analogues

• Lucie Brulikova and
• Jan Hlavac

Beilstein J. Org. Chem. 2011, 7, 678–698, doi:10.3762/bjoc.7.80

• obtained from clinical material of patients treated at the University Hospital in Olomouc (methicillin resistant Staphylococcus aureus - MRSA, Staphylococcus haemolyticus, Escherichia coli and Pseudomonas aeruginosa) with resistance to currently used fluoroquinolones. Only the octyl and nonyl derivatives

• 126h, 127h and 126i, 127i showed slight activity against Enterococcus faecalis CCM 4224, Staphylococcus aureus CCM 3953, Staphylococcus aureus (MRSA) and Staphylococcus haemolyticus. Conclusion This review was an attempt to summarize all available information on the synthesis and biological activity of