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A synthetic methodology to afford unusual glycoconjugate building blocks useful for the solid-phase synthesis of C-linked antifreeze glycoprotein (AFGP) analogues is described. Such compounds are urgently required in order to elucidate the molecular mechanism by which AFGPs function. All reactions are general in nature and accommodate structural variation in the carbohydrate moiety, polypeptide backbone, and amino acid side chain. 相似文献
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Rafika Brakni Monia Ali Ahmed Pauline Burger Aurélie Schwing Grégory Michel Christelle Pomares Lillia Hasseine Laurent Boyer Xavier Fernandez Anne Landreau Thomas Michel 《化学与生物多样性》2018,15(4)
Lichens are complex symbiotic organisms able to produce a vast array of compounds. The Algerian lichen diversity has only prompted little interest even given the 1085 species listed. Herein, the chemodiversity of four Algerian lichens including Cladonia rangiformis, Ramalina farinaceae, R. fastigiata, and Roccella phycopsis was investigated. A dereplication strategy, using ultra high performance liquid chromatography‐high resolution‐electrospray ionization‐mass spectrometry (UHPLC‐HRMS/MS), was carried out for a comprehensive characterization of their substances including phenolics, depsides, depsidones, depsones, dibenzofurans, and aliphatic acids. Some known compounds were identified for the first time in some species. Additionally, the lichenic extracts were evaluated for their antifungal and antimicrobial activities on human pathogenic strains (Candida albicans, C. glabrata, Aspergillus fumigatus, Staphylococcus aureus, and Escherichia coli). Cyclohexane extracts were found particularly active against human pathogenic fungi with MIC80 values ranging from 8 to 62.5 μg/mL, without cytotoxicity. This study highlights the therapeutic and prophylactic potential of lichenic extracts as antibacterial and antifungal agents. 相似文献
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Chevreuil F Landreau A Seraphin D Larcher G Bouchara JP Richomme P 《Journal of enzyme inhibition and medicinal chemistry》2008,23(5):617-622
New 1-[2-azido-2-(2,4-dichlorophenyl)ethyl]-1H/-imidazole were synthesized by nucleophilic substitution of various tertiary alcohols with azide anion in presence of boron trifluoride-diethyl etherate. Their antifungal activity was evaluated against Candida albicans, Candida glabrata, Aspergillus fumigatus and an azole-resistant petite mutant of C. glabrata. Preliminary SAR results are discussed. 相似文献
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Samuel Bertrand Gérald Larcher Anne Landreau Pascal Richomme Olivier Duval Jean-Philippe Bouchara 《Biometals》2009,22(6):1019-1029
Scedosporium apiospermum is an emerging pathogen colonizing the airways of patients with cystic fibrosis and causing severe infections in immunocompromised
hosts. In order to improve our knowledge on the pathogenic mechanisms of this fungus, we investigated the production of siderophores.
Cultivation on CAS medium and specific assays for different classes of siderophores suggested the secretion of hydroxamates.
A maximal production was obtained by cultivation of the fungus at alkaline pH in an iron-restricted liquid culture medium.
Siderophores were then extracted from the culture filtrate by liquid/liquid extraction, and separated by reverse phase high
performance liquid chromatography. Two siderophores, dimerumic acid and N
α-methyl coprogen B, were identified by electrospray ionization-mass spectrometry and MS–MS fragmentation. Finally, comparison
of various strains suggested a higher production of N
α-methyl coprogen B by clinical isolates of respiratory origin. Studies are initiated in order to determine the potential usefulness
of these siderophores as diagnostic markers of scedosporiosis. 相似文献
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Francis Chevreuil Anne Landreau Gérald Larcher Jean-Philippe Bouchara Pascal Richomme 《Journal of enzyme inhibition and medicinal chemistry》2013,28(5):617-622
New 1-[2-azido-2-(2,4-dichlorophenyl)ethyl]-1H/-imidazole were synthesized by nucleophilic substitution of various tertiary alcohols with azide anion in presence of boron trifluoride-diethyl etherate. Their antifungal activity was evaluated against Candida albicans, Candida glabrata, Aspergillus fumigatus and an azole-resistant petite mutant of C. glabrata. Preliminary SAR results are discussed. 相似文献
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Sylvie Morel Jean-Jacques Helesbeux Denis Séraphin Séverine Derbré Julia Gatto Marie-Christine Aumond Yannick Abatuci Philippe Grellier Mehdi A. Beniddir Patrice Le Pape Fabrice Pagniez Marc Litaudon Anne Landreau Pascal Richomme 《Phytochemistry letters》2013,6(3):498-503
A new isoflavonoid, 5-hydroxy-3-(4-hydroxyphenyl)-8-isopropenyl-8,9-dihydro-4H-furo-[2,3-h]-chromen-4-one named derrisisoflavone G (1), four known prenylated flavanones (2–5), four known isoflavonoids (6–9) and two phenolic derivatives (10, 11) have been isolated from crude extracts of Derris ferruginea stems and leaves. Compounds 1–11 were identified using spectroscopic methods whereas an unambiguous structural assignment of 1 was accomplished through hemi-synthesis. Compounds 2–5 exhibited strong in vitro antiparasitic activity against Plasmodium falciparum and Leishmania major but with poor selectivity, whereas 1–5 significantly inhibited the formation of advanced glycation endproducts (AGEs). 相似文献
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Pinel B Landreau A Seraphin D Larcher G Bouchara JP Richomme P 《Journal of enzyme inhibition and medicinal chemistry》2005,20(6):575-579
Abstract The synthesis of new xanthanolide derivatives is reported starting from xanthatin, a sesquiterpenic lactone isolated from Xanthium macrocarpum (Asteraceae). In vitro evaluation of their antifungal activity has been investigated. 相似文献