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Lipophosphonoxins: New Modular Molecular Structures with Significant Antibacterial Properties
- 1.0367626 - ÚOCHB 2012 RIV US eng J - Journal Article
Rejman, Dominik - Rabatinová, Alžběta - Pombinho, António R. - Kovačková, Soňa - Pohl, Radek - Zborníková, Eva - Kolář, M. - Bogdanová, K. - Nyč, O. - Šanderová, Hana - Látal, T. - Bartůněk, Petr - Krásný, Libor
Lipophosphonoxins: New Modular Molecular Structures with Significant Antibacterial Properties.
Journal of Medicinal Chemistry. Roč. 54, č. 22 (2011), s. 7884-7898. ISSN 0022-2623. E-ISSN 1520-4804
R&D Projects: GA MŠMT(CZ) LC06077; GA ČR GA204/09/0583; GA ČR GAP302/11/0855; GA MŠMT 2B06065
Institutional research plan: CEZ:AV0Z40550506; CEZ:AV0Z50200510; CEZ:AV0Z50520514
Keywords : lipofosfonoxin * antibacterial * nucleoside
Subject RIV: CC - Organic Chemistry
Impact factor: 5.248, year: 2011
Novel compounds termed lipophosphonoxins were prepared using a simple and efficient synthetic approach. The general structure of lipophosphonoxins consists of four modules: (i) a nucleoside module, (ii) an iminosugar module, (iii) a hydrophobic module (lipophilic alkyl chain), and (iv) a phosphonate linker module that holds together modules i–iii. Lipophosphonoxins displayed significant antibacterial properties against a panel of Gram-positive species, including multiresistant strains. The minimum inhibitory concentration (MIC) values of the best inhibitors were in the 1–12 .mu.g/mL range, while their cytotoxic concentrations against human cell lines were significantly above this range. The modular nature of this artificial scaffold offers a large number of possibilities for further modifications/exploitation of these compounds.
Permanent Link: http://hdl.handle.net/11104/0202228
Number of the records: 1