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5-benzylidenethiazolidin-4-ones as multitarget inhibitors of bacterial Mur ligases
Tomašič, Tihomir (Author), Zidar, Nace (Author), Kovač, Andreja (Author), Turk, Samo (Author), Simčič, Mihael (Author), Blanot, Didier (Author), Müller-Premru, Manica (Author), Filipič, Metka (Author), Golič Grdadolnik, Simona (Author), Zega, Anamarija (Author), Anderluh, Marko (Author), Gobec, Stanislav (Author), Kikelj, Danijel (Author), Peterlin-Mašič, Lucija (Author)

URLURL - Presentation file, Visit http://www3.interscience.wiley.com/journal/123218167/abstract This link opens in a new window

Abstract
Mur ligases participate in the intracellular path of bacterial peptidoglycan biosynthesis and constitute attractive, although so far underexploited, targets for antibacterial drug discovery. A series of hydroxy-substituted 5-benzylidenethiazolidin-4-ones were synthesized and tested as inhibitors of Mur ligases. The most potent compound 5 a was active against MurD-F with IC50 values between 2 and 6 m, making it a promising multitarget inhibitor of Mur ligases. Antibacterial activity against different strains, inhibitory activityagainst protein kinases, mutagenicity and genotoxicity of 5 a were also investigated, and kinetic and NMR studies were conducted.

Language:English
Keywords:inhibitorji, Mur ligaze, NMR proteini, tiazolidini
Work type:Not categorized (r6)
Tipology:1.01 - Original Scientific Article
Organization:FFA - Faculty of Pharmacy
Year:2010
Number of pages:str. 286-295
Numbering:Vol. 5, iss. 2
UDC:543+542
ISSN on article:1860-7179
COBISS.SI-ID:2743921 Link is opened in a new window
Views:635
Downloads:182
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Record is a part of a journal

Title:ChemMedChem
Publisher:Wiley-VCH Verlag GmbH
ISSN:1860-7179
COBISS.SI-ID:27051781 This link opens in a new window

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