- Exploring intermolecular contacts in multi-substituted benzaldehyde derivatives: X-ray, Hirshfeld surface and lattice energy analyses
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Crystal structures of six benzaldehyde derivatives (1-6) have been determined and their supramolecular networks were established by an X-ray crystallographic study. The study has shown that the compounds are linked by various intermolecular interactions s
- Hosten, Eric C.,Hulushe, Siya T.,Louzada, Marcel,Manyeruke, Meloddy H.,Rigin, Sergei,Watkins, Gareth M.
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p. 16861 - 16874
(2020/05/18)
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- SAR Studies on Aromatic Acylhydrazone-Based Inhibitors of Fungal Sphingolipid Synthesis as Next-Generation Antifungal Agents
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Recently, the fungal sphingolipid glucosylceramide (GlcCer) synthesis has emerged as a highly promising new target for drug discovery of next-generation antifungal agents, and we found two aromatic acylhydrazones as effective inhibitors of GlcCer synthesis based on HTP screening. In the present work, we have designed libraries of new aromatic acylhydrazones, evaluated their antifungal activities (MIC80 and time-kill profile) against C. neoformans, and performed an extensive SAR study, which led to the identification of five promising lead compounds, exhibiting excellent fungicidal activities with very large selectivity index. Moreover, two compounds demonstrated broad spectrum antifungal activity against six other clinically relevant fungal strains. These five lead compounds were examined for their synergism/cooperativity with five clinical drugs against seven fungal strains, and very encouraging results were obtained; e.g., the combination of all five lead compounds with voriconazole exhibited either synergistic or additive effect to all seven fungal strains.
- Del Poeta, Maurizio,Haranahalli, Krupanandan,Lazzarini, Cristina,Mallamo, John,McCarthy, J. Brian,Ojima, Iwao,Pathiranage, Senuri,Sun, Yi,Zambito, Julia
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- Electrophilic carbon transfer in gold catalysis: Synthesis of substituted chromones
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Using easily accessible aromatic alkoxy-arylalkynones, we have investigated the gold-catalyzed intramolecular addition of ethers to alkynes, to give easy access to various substituted chromones. This reaction involves the transfer of the ether substituent via a carbodemetallation process. We also noticed a competing isomerization of several starting materials for which we propose a second gold catalyzed mechanism.
- Renault, Jacques,Qian, Zhao,Uriac, Philippe,Gouault, Nicolas
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supporting information; experimental part
p. 2476 - 2479
(2011/05/16)
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- A convenient and improved Baylis-Hillman synthesis of 3-substututed 2H-1-benzopyran-2-ones
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Halogen acid-catalysed deprotection and cyclisation of Baylis-Hillman products obtained using O-benzylated salicylaldehyde precursors has been shown to afford 3-(halomethyl)coumarins (3-halomethyl-2H-1-benzopyran-2-ones) chemoselectively and in good yield.
- Kaye, Perry T.,Musa, Musiliyu A.
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p. 2701 - 2706
(2007/10/03)
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