Design of a novel tryptophan-rich membrane-active antimicrobial peptide from the membrane-proximal region of the HIV glycoprotein, gp41

• Evan F. Haney,
• Leonard T. Nguyen,
• David J. Schibli and
• Hans J. Vogel

Beilstein J. Org. Chem. 2012, 8, 1172–1184, doi:10.3762/bjoc.8.130

• with the greatest degree of amphipathicity and largest positive charge proved to be the most potent antimicrobial, and this peptide could be further modified to improve the antimicrobial activity. However, the other two peptides were relatively ineffective antimicrobials and instead proved to be

• that does not possess intrinsic antimicrobial activity. Peptides derived from the envelope HIV-1 glycoproteins, gp120 and gp41, have previously been examined for their antimicrobial activity [10] and we chose to use the membrane-proximal region of gp41 as our starting peptide scaffold. This region of

• potent antimicrobial activity. Three derivatives were synthesized based on the amino-acid sequence of gp41w (Figure 1). The first peptide, gp41w-4R, has the polar uncharged amino acids in gp41w replaced with Arg residues. These mutations increased the net charge of the peptide from +3 to +7 and should

Algicidal lactones from the marine Roseobacter clade bacterium Ruegeria pomeroyi

• Ramona Riclea,
• Julia Gleitzmann,
• Hilke Bruns,
• Corina Junker,
• Barbara Schulz and
• Jeroen S. Dickschat

Beilstein J. Org. Chem. 2012, 8, 941–950, doi:10.3762/bjoc.8.106

• ) under reflux for 6 h gave a mixture of (2R,4S)-7 and (2S,4S)-8, which was used for enantioselective GC analyses. Agar diffusion assay for antimicrobial activity. The substances were dissolved in MeOH at a concentration of 2 mg/mL. Twenty-five microlitres of the solutions (equal to 50 μg of the compounds

Phytoalexins of the Pyrinae: Biphenyls and dibenzofurans

• Cornelia Chizzali and
• Ludger Beerhues

Beilstein J. Org. Chem. 2012, 8, 613–620, doi:10.3762/bjoc.8.68

• after treatment with biotic and abiotic elicitors. The antimicrobial activity of the phytoalexins was demonstrated. To date, 10 biphenyls and 17 dibenzofurans were isolated from 14 of the 30 Pyrinae genera. The most widely distributed compounds are the biphenyl aucuparin and the dibenzofuran γ

Synthesis and characterization of new diiodocoumarin derivatives with promising antimicrobial activities

• Hany M. Mohamed,
• Ashraf H. F. Abd EL-Wahab,
• Ahmed M. EL-Agrody,
• Ahmed H. Bedair,
• Fathy A. Eid,
• Mostafa M. Khafagy and
• Kamal A. Abd-EL-Rehem

Beilstein J. Org. Chem. 2011, 7, 1688–1696, doi:10.3762/bjoc.7.199

• ethyl 4-oxo-2,6-methano-2-methyl-3,4,5,6-tetrahydro-8,10-diiodobenzo[2,1-g]-2H-1,3-oxazocine-5-carboxylate derivatives 14a,b. All compounds were evaluated for their antimicrobial activity and the compounds 12–14a,b exhibited a pronounced effect on all tested microorganisms. Keywords: antimicrobial; 3,5

• measured in millimeters (6 mm) at the end of an incubation period of 48 h at 28 °C; N,N-dimethylformamide showed no inhibition zone. Conclusion It was interesting to note that four of the new compounds (12, 13 and 14a,b) were found to have an antimicrobial activity greater than that of the standard

• antibiotic ampicillin or the standard antifungal claforan, while compounds 1–11 were either inactive or only weakly active against the tested microorganisms. The presence of fused diiodocoumarino[3,4-c]pyridine and diiodobenzo[2,1-g]-2H-1,3-oxazocine nucleus increased the antimicrobial activity, whereas the

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

• longer alkynyl chains might be a successful way to obtain potentially active antimycobacterial drugs. Recently, the antimicrobial activity of 5-[alkoxy-(4-nitrophenyl)methyl]uridines 126, 127 has been studied [35]. Eight isomers with different alkyl side chain lengths, 126 and 127 (Figure 20), were

• tested for their antimicrobial activity against standard reference gram-positive and gram-negative bacterial strains such as Enterococcus faecalis CCM 4224, Staphylococcus aureus CCM 3953, Escherichia coli CCM 3954 and Pseudomonas aeruginosa CCM 3955 and against gram-positive and gram-negative bacteria

SbCl₃-catalyzed one-pot synthesis of 4,4′-diaminotriarylmethanes under solvent-free conditions: Synthesis, characterization, and DFT studies

• Ghasem Rezanejade Bardajee

Beilstein J. Org. Chem. 2011, 7, 135–144, doi:10.3762/bjoc.7.19

• [11][12][13], antitubercular [14], anti-infective, and antimicrobial activity [15]. Additionally, they have been used for sterilization of trypanosome cruizi-infected blood [16], in biotechnology process control [17][18], in dye-assisted laser inactivation of enzymes [19], in wastewater treatment

Pyridinium based amphiphilic hydrogelators as potential antibacterial agents

• Sayanti Brahmachari,
• Sisir Debnath,
• Sounak Dutta and
• Prasanta Kumar Das

Beilstein J. Org. Chem. 2010, 6, 859–868, doi:10.3762/bjoc.6.101

• (λ = 0.15406 nm) with a voltage and current of 40 kV and 30 mA, respectively. The gel was mounted on a glass slide and dried under vaccum. The xerogel was scanned from 2Θ = 1–40°. Microorganisms and culture conditions The in vitro antimicrobial activity of the cationic amphiphiles was investigated