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5-benzylidenethiazolidin-4-ones as multitarget inhibitors of bacterial Mur ligasesTomašič, Tihomir ...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.Vir: ChemMedChem : Chemistry Enabling Drug Discovery. - ISSN 1860-7179 (Vol. 5, iss. 2, 2010, str. 286-295)Vrsta gradiva - članek, sestavni delLeto - 2010Jezik - angleškiCOBISS.SI-ID - 2743921
Avtor
Tomašič, Tihomir |
Zidar, Nace |
Kovač, Andreja, farmacevtka, 1979- |
Turk, Samo |
Simčič, Mihael |
Blanot, Didier |
Müller-Premru, Manica |
Filipič, Metka, 1954- |
Golič Grdadolnik, Simona |
Zega, Anamarija |
Anderluh, Marko |
Gobec, Stanislav, 1970- |
Kikelj, Danijel |
Peterlin-Mašič, Lucija
Teme
inhibitorji |
Mur ligaze |
NMR proteini |
tiazolidini
Vnos na polico
Trajna povezava
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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Tomašič, Tihomir | 28334 |
Zidar, Nace | 28905 |
Kovač, Andreja, farmacevtka, 1979- | 27782 |
Turk, Samo | 29773 |
Simčič, Mihael | 28554 |
Blanot, Didier | |
Müller-Premru, Manica | 12193 |
Filipič, Metka, 1954- | 09892 |
Golič Grdadolnik, Simona | 08329 |
Zega, Anamarija | 18633 |
Anderluh, Marko | 21456 |
Gobec, Stanislav, 1970- | 15284 |
Kikelj, Danijel | 01463 |
Peterlin-Mašič, Lucija | 19317 |
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