Triterpenoid saponins from the roots of Acanthophyllum gypsophiloides Regel

• Elena A. Khatuntseva,
• Vladimir M. Men’shov,
• Alexander S. Shashkov,
• Yury E. Tsvetkov,
• Rodion N. Stepanenko,
• Raymonda Ya. Vlasenko,
• Elvira E. Shults,
• Genrikh A. Tolstikov,
• Tatjana G. Tolstikova,
• Dimitri S. Baev,
• Vasiliy A. Kaledin,
• Nelli A. Popova,
• Valeriy P. Nikolin,
• Pavel P. Laktionov,
• Anna V. Cherepanova,
• Tatiana V. Kulakovskaya,
• Ekaterina V. Kulakovskaya and
• Nikolay E. Nifantiev

Beilstein J. Org. Chem. 2012, 8, 763–775, doi:10.3762/bjoc.8.87

• obtained saponins were elucidated by a combination of mass spectrometry and 2D NMR spectroscopy. A study of acute toxicity, hemolytic, anti-inflammatory, immunoadjuvant and antifungal activity was carried out. Both saponins 1 and 2 were shown to exhibit immunoadjuvant properties within the vaccine

• : Basidiomycetous yeasts Cryptococcus terreus, Filobasidiella neoformans, and ascomycetous yeasts Saccharomyces cerevisiae and Саndida albicans. The data in Table 7 demonstrate that compounds 1 and 2 exhibit antifungal activity against both ascomycetous and basidiomycetous yeasts, including the medically important

• C. albicans and F. neoformans. Saponins are known to be more effective against basidiomycetous yeast and at acidic pH act similarly to natural detergents, such as cellobiose lipids [27]. Growth inhibition experiments showed (Figure 6, Table 7), that the lower pH 4.0 favored antifungal activity of

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

• by microorganisms or herbivores and provide a constitutive barrier. Antimicrobial properties Antifungal activity of biphenyls and dibenzofurans was demonstrated in a number of studies [4][7][8][9][10][12][13][14][15][18][19][21]. Spore germination, germ-tube development, and mycelial growth were

• ) were tested for their inhibitory effect on the scab-causing fungus, Venturia inaequalis, the aglycone exhibited significantly stronger antifungal activity than the glucoside [10]. This finding agrees with the observation that the accumulated phytoalexins are commonly aglycones of biphenyls and

• did [12], whereas the opposite tendency was observed for antifungal activity [26]. However, more biphenyls and dibenzofurans need to be tested for their antibacterial and antifungal potentials in order to allow for reliable conclusions concerning structure–activity relationships. The array of

Synthesis of szentiamide, a depsipeptide from entomopathogenic Xenorhabdus szentirmaii with activity against Plasmodium falciparum

• Friederike I. Nollmann,
• Andrea Dowling,
• Marcel Kaiser,
• Klaus Deckmann,
• Sabine Grösch,
• Richard ffrench-Constant and
• Helge B. Bode

Beilstein J. Org. Chem. 2012, 8, 528–533, doi:10.3762/bjoc.8.60

• different Gram-positive (Micrococcus luteus, Bacillus subtilis, Staphylococcus aureus) and Gram-negative (Escherichia coli, Pseudomonas aeroginosa) bacteria, as well as yeast (Candida albicans, Saccharomyces cerivisiae). However, consistent with the published data [12], no antibacterial or antifungal

• activity was detected. Additionally, the peptide 1 was tested against several parasites (Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani, Plasmodium falciparum) being the causative agents of the neglected tropical diseases [18] sleeping sickness, leishmaniasis and malaria

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

• activity against the tested organisms. Compounds 9–11 exhibited comparable activity to ampicillin against the tested bacteria and moderate to weak antifungal activity against the tested organisms. Furthermore, compounds 1–8 showed moderate to weak activities against all the tested bacteria and fungi

• ampicillin (30 µg mL−1) as the standard antibiotic reference for antibacterial activity, and calforan (30 µg mL−1) was used as a reference antifungal activity. The tested compounds were dissolved in N,N-dimethylformamide (DMF) to give a solution of 1 mg mL−1. The inhibition zones (diameter of the hole) were

• presence of diiodocoumarin-3-carboxamides decreased the antimicrobial activity. Graphical representation of the antibacterial activity of tested compounds compared to ampicillin. Graphical representation of antifungal activity of tested compounds, compared to calforan. Synthesis of 6,8-diiodocoumarin

Natural product biosyntheses in cyanobacteria: A treasure trove of unique enzymes

• Jan-Christoph Kehr,
• Douglas Gatte Picchi and
• Elke Dittmann

Beilstein J. Org. Chem. 2011, 7, 1622–1635, doi:10.3762/bjoc.7.191

• ]. Hectochlorin Hectochlorin (10) was isolated from a Jamaican isolate of Lyngbya majuscula and exhibits antifungal activity. It also shows potent activity towards a number of cancer cell lines. HctA, an acyl-CoA synthetase homologue, is expected to activate free hexanoic acid and to provide the starter for

Advances in synthetic approach to and antifungal activity of triazoles

• Kumari Shalini,
• Nitin Kumar,
• Sushma Drabu and
• Pramod Kumar Sharma

Beilstein J. Org. Chem. 2011, 7, 668–677, doi:10.3762/bjoc.7.79

• that bioisosteric replacement of a triazole ring leads to antifungal activity with a higher selectivity of the fungal targets. Triazole antifungal drugs are used in the treatment of both superficial and deep-seated candidiasis [30]. On the basis of various literature surveys, the triazole nucleus

• occupies the most important place in the treatment of fungal diseases. The triazole derivatives noted below were synthesized by various groups and show antifungal activity. Novel 1,2,3-triazole-linked with β-lactam–bile acid conjugates were prepared via 1,3-dipolar cycloaddition reactions of azido β

• -lactams and terminal alkynes of bile acids in the presence of a Cu(I) catalyst (click chemistry) by Vatmurge et al. The synthesized compounds were evaluated for their antifungal activity against different fungal strains such as Candida albicans, Cryptococcus neoformans, Benjaminiella poitrasii, Yarrowia

First synthesis of 2-(benzofuran-2-yl)-6,7-methylene dioxyquinoline-3-carboxylic acid derivatives

• Wentao Gao,
• Jia Liu,
• Yun Jiang and
• Yang Li

Beilstein J. Org. Chem. 2011, 7, 210–217, doi:10.3762/bjoc.7.28

• reported to inhibit C. albicans prolyl-tRNA synthetase and displayed potent in vitro antifungal activity against dermatophytes [6]. Consequently, studies concerning novel 2-heteroarylquinoline derivatives appear frequently in the literature [7][8]. In a nature’s collection of biologically active

Approaches towards the synthesis of 5-aminopyrazoles

• Ranjana Aggarwal,
• Vinod Kumar,
• Rajiv Kumar and
• Shiv P. Singh

Beilstein J. Org. Chem. 2011, 7, 179–197, doi:10.3762/bjoc.7.25

• mammalian receptors [10]. The simple N-phenyl amide of 5-amino -1,3-dimethylpyrazole-4-carboxylic acid V has been shown to exhibit antifungal activity [11] (Figure 1). The 5-amino-1-pyrazinyl-3-carboxamidopyrazole derivative VI has been recently reported as a potent antibacterial agent with a very broad

Synthesis of some novel hydrazono acyclic nucleoside analogues

• Mohammad N. Soltani Rad,
• Ali Khalafi-Nezhad and
• Somayeh Behrouz

Beilstein J. Org. Chem. 2010, 6, No. 49, doi:10.3762/bjoc.6.49

• been an increase in the number of antifungal drugs available with various structures and scaffolds. However, their clinical value has been limited by the emergence of drug resistance, high risk of toxicity, insufficiencies in their antifungal activity as well as undesirable side effects. This situation