103754-57-0Relevant articles and documents
Benzoxazolyl linked benzylidene based rhodanine and analogs as novel antidiabetic agents: synthesis, molecular docking, and in vitro studies
Singh, Varinder,Singh, Amanjot,Singh, Gagandeep,Verma, Raman K.,Mall, Rajiv
, p. 1905 - 1914 (2021)
Benzoxazolyl linked meta- and para-substituted new chemical entities (5a–5h) featuring thiazolidinedione, rhodanine, hydantoin, and thiohydantoin moieties were synthesized and characterized by 1H NMR, 13C NMR, FT-IR, and HRMS spectra
Substituent and solvent effects on intramolecular charge transfer of 5-arylidene-2,4-thiazolidinediones
Ran?i?, Milica,Tri?ovi?, Nemanja,Mil?i?, Milo?,U??umli?, Gordana,Marinkovi?, Aleksandar
experimental part, p. 500 - 507 (2012/02/04)
The absorption spectra of twelve 5-arylidene-2,4-thiazolidinediones were recorded in twenty one solvents in the range from 300 to 600 nm. The effect of specific and non-specific solvent-solute interactions on the absorption maxima shifts were evaluated by
Structure-based design of a new series of d-glutamic acid based inhibitors of bacterial UDP-N-acetylmuramoyl-l-alanine: D-glutamate ligase (MurD)
Toma?i?, Tihomir,Zidar, Nace,?ink, Roman,Kova?, Andreja,Blanot, Didier,Contreras-Martel, Carlos,Dessen, Andréa,Müller-Premru, Manica,Zega, Anamarija,Gobec, Stanislav,Kikelj, Danijel,Peterlin Ma?i?, Lucija
supporting information; experimental part, p. 4600 - 4610 (2011/09/14)
MurD ligase is one of the key enzymes participating in the intracellular steps of peptidoglycan biosynthesis and constitutes a viable target in the search for novel antibacterial drugs to combat bacterial drug-resistance. We have designed, synthesized, and evaluated a new series of d-glutamic acid-based Escherichia coli MurD inhibitors incorporating the 5-benzylidenethiazolidin-4- one scaffold. The crystal structure of 16 in the MurD active site has provided a good starting point for the design of structurally optimized inhibitors 73-75 endowed with improved MurD inhibitory potency (IC50 between 3 and 7 μM). Inhibitors 74 and 75 showed weak activity against Gram-positive Staphylococcus aureus and Enterococcus faecalis. Compounds 73-75, with IC 50 values in the low micromolar range, represent the most potent d-Glu-based MurD inhibitors reported to date.
Discovery of novel 5-benzylidenerhodanine and 5-benzylidenethiazolidine-2, 4-dione inhibitors of MurD ligase
Zidar, Nace,Toma?i?, Tihomir,?ink, Roman,Rupnik, Veronika,Kova?, Andreja,Turk, Samo,Patin, Delphine,Blanot, Didier,Contreras Martel, Carlos,Dessen, Andréa,Müller Premru, Manica,Zega, Anamarija,Gobec, Stanislav,Peterlin Ma?i?, Lucija,Kikelj, Danijel
supporting information; experimental part, p. 6584 - 6594 (2010/11/17)
We have designed, synthesized, and evaluated 5-benzylidenerhodanine-and 5-benzylidenethiazolidine-2,4-dione-based compounds as inhibitors of bacterial enzyme MurD with E. coli IC50 in the range 45-206 μM. The high-resolution crystal structure o
Synthesis and biological evaluation of new glutamic acid-based inhibitors of MurD ligase
Tomasic, Tihomir,Zidar, Nace,Rupnik, Veronika,Kovac, Andreja,Blanot, Didier,Gobec, Stanislav,Kikelj, Danijel,Masic, Lucija Peterlin
scheme or table, p. 153 - 157 (2009/05/07)
Mur ligases catalyze the biosynthesis of the UDP-MurNAc-pentapeptide precursor of peptidoglycan, an essential polymer of bacterial cell-wall. They constitute attractive targets for the development of novel antibacterial agents. Here we report on the synth
Structure-activity relationships and molecular modelling of 5-arylidene-2,4-thiazolidinediones active as aldose reductase inhibitors
Maccari, Rosanna,Ottana, Rosaria,Curinga, Carmela,Vigorita, Maria Gabriella,Rakowitz, Dietmar,Steindl, Theodora,Langer, Thierry
, p. 2809 - 2823 (2007/10/03)
The structure-activity relationships (SARs) of 5-arylidene-2,4- thiazolidinediones active as aldose reductase inhibitors (ARIs) were extended by varying the substitution pattern on the 5-arylidene moiety and on N-3. In particular, the introduction of an a
