Search results for "antifungal agents"
showing 10 items of 229 documents
Synthesis and biological evaluation of (+)-labdadienedial, derivatives and precursors from (+)-sclareolide
2010
Labdadienedial and a series of C15,C16-functionalized derivatives were synthesized from commercial (+)-sclareolide and evaluated for their cytotoxic, antimycotic, and antiviral activities. Their precursors were similarly evaluated.
Steroidal saponins from Asparagus acutifolius.
2007
Abstract Six new steroidal saponins ( 1 – 6 ) were isolated from the roots of A. acutifolius L., together with a known spirostanol glycoside ( 7 ). Their structures were elucidated mainly by extensive spectroscopic analysis (1D and 2D NMR, FABMS and HRESIMS). Compounds 4 – 7 demonstrated antifungal activity against the human pathogenic yeasts C. albicans , C. glabrata and C. tropicalis with MICs values between 12.5 and 100 μg/ml.
Synthesis and antimicrobial activity of new 3-(1-R-3(5)-methyl-4-nitroso-1H-5(3)-pyrazolyl)-5-methylisoxazoles.
2000
A number of new 3-(1-R-3(5)-methyl-4-nitroso-1H-5(3)-pyrazolyl)-5-methylisoxazoles 6a-g (7b-f) were synthesized and tested for antibacterial and antifungal activity. Some of these compounds displayed antifungal activity at non-cytotoxic concentrations. Derivative 6c was 9 times more potent in vitro than miconazole and 20 times more selective against C. neoformans. 6c was also 8- and 125-fold more potent than amphotericin B and fluconazole, respectively. None of the compounds was active against bacteria. Preliminary structure-activity relationship (SAR) studies showed that the NO group at position 4 of the pyrazole ring is essential for the activity. Lipophilicity of the pyrazole moiety, N-a…
Steroidal saponins from Smilax medica and their antifungal activity.
2005
Three new steroidal saponins (1-3) were isolated from the roots of Smilax medica, together with the known disporoside A (4). The structures of the new compounds were elucidated mainly by extensive spectroscopic analysis (1D and 2D NMR, FABMS, and HRESIMS). Compounds 1, 2, and 4 demonstrated weak antifungal activity against the human pathogenic yeasts Candida albicans, C. glabrata, and C.tropicalis, with MIC values between 12.5 and 50 microg/mL.
Synthesis and Influence of 3-Amino Benzoxaboroles Structure on Their Activity against Candida albicans
2020
Benzoxaboroles emerged recently as molecules of high medicinal potential with Kerydin®
Mechanisms of nanotoxicity – biomolecule coronas protect pathological fungi against nanoparticle-based eradication
2020
Whereas nanotoxicity is intensely studied in mammalian systems, our knowledge of desired or unwanted nano-based effects for microbes is still limited. Fungal infections are global socio-economic health and agricultural problems, and current chemical antifungals may induce adverse side-effects in humans and ecosystems. Thus, nanoparticles are discussed as potential novel and sustainable antifungals via the desired nanotoxicity but often fail in practical applications. In our study, we found that nanoparticles' toxicity strongly depends on their binding to fungal spores, including the clinically relevant pathogen
Pga13 in Candida albicans is localized in the cell wall and influences cell surface properties, morphogenesis and virulence.
2011
The fungal cell wall is an essential organelle required for maintaining cell integrity and also plays an important role in the primary interactions between pathogenic fungi and their hosts. PGA13 encodes a GPI protein in the human pathogen Candida albicans, which is highly up-regulated during cell wall regeneration in protoplasts. The Pga13 protein contains a unique tandem repeat, which is present five times and is characterized by conserved spacing between the four cysteine residues. Furthermore, the mature protein contains 38% serine and threonine residues, and therefore probably is a highly glycosylated cell wall protein. Consistent with this, a chimeric Pga13-V5 protein could be localiz…
A kinetic study on the regeneration ofCandida albicansprotoplasts in the presence of cell wall synthesis inhibitors
1993
Aculeacin A and papulacandin B block cell wall regeneration in Candida albicans protoplasts at an intermediate step in which the protoplasts have not yet synthesized the rigid structure of the cell wall and are therefore still osmotically sensitive. In the presence of the antibiotics, total synthesis of glucan is not significantly lowered with respect to control cells, although most of it appears either in the culture medium or in the regenerating wall as alkali-soluble glucan. Thus, it is proposed that echinocandins (such as aculeacin A) and papulacandins may not inhibit glucan synthesis per se but instead inhibit its incorporation into the supramolecular organization of the cell wall.
A role for the MAP kinase gene MKC1 in cell wall construction and morphological transitions in Candida albicans.
1998
The Candida albicans MKC1 gene encodes a mitogen-activated protein (MAP) kinase, which has been cloned by complementation of the lytic phenotype associated with Saccharomyces cerevisiae slt2 (mpk1) mutants. In this work, the physiological role of this MAP kinase in the pathogenic fungus C. albicans was characterized and a role for MKC1 in the biogenesis of the cell wall suggested based on the following criteria. First, C. albicans mkc1Δ/mkc1Δ strains displayed alterations in their cell surfaces under specific conditions as evidenced by scanning electron microscopy. Second, an increase in specific cell wall epitopes (O-glycosylated mannoprotein) was shown by confocal microscopy in mkc1Δ/mkc1…