A series of 3-amino- and polyaminosterol analogues of squalamine and trodusquemine were synthesized and evaluated for their in vitro antimicrobial properties against human pathogens. The activity was highly dependent on the structure of the different compounds involved and the best results were obtained with aminosterol derivatives 4b, 4e, 8b, 8e and 8n exhibiting minimum inhibitory concentrations (MICs) against yeasts, Gram positive and Gram negative bacteria at average concentrations of 3.12-12.5 microM.
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http://dx.doi.org/10.1080/14756360701809910 | DOI Listing |
J Enzyme Inhib Med Chem
December 2008
Laboratoire SESNAB, UMR-MD1, case 342, Faculté de St Jérome, Université de Méditerranée, Marseille, Cedex 20, France.
A series of 3-amino- and polyaminosterol analogues of squalamine and trodusquemine were synthesized and evaluated for their in vitro antimicrobial properties against human pathogens. The activity was highly dependent on the structure of the different compounds involved and the best results were obtained with aminosterol derivatives 4b, 4e, 8b, 8e and 8n exhibiting minimum inhibitory concentrations (MICs) against yeasts, Gram positive and Gram negative bacteria at average concentrations of 3.12-12.
View Article and Find Full Text PDFEur J Med Chem
March 2008
Laboratoire SESNAB, Biosciences, UMR-MD-1, case 342, Faculté de St Jérôme, Université Paul Cézanne, Av. Escadrille Normandie Niemen, 13397 Marseille, Cedex 20, France.
A series of 3-amino and polyaminosterol analogues of squalamine and trodusquemine were synthesized involving a new stereoselective titanium reductive amination reaction in high chemical yields of up to 95% in numerous cases. These derivatives were evaluated for their in vitro antimicrobial properties against human pathogens. Activity was highly dependent on the different compounds' structures involved and best results have been obtained with aminosterol derivatives 4b, 4e and 6i exhibiting activities against yeasts, Gram positive and Gram negative bacteria at average concentrations of 6.
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