2644-96-4Relevant articles and documents
Dissociation of amides in strongly basic medium of sodium methoxide in dimethyl sulfoxide-methanol mixtures
Mitas, Petr,Kavalek, Jaromir,Pytela, Oldrich
, p. 1562 - 1576 (1997)
The dissociation constants of eleven amides have been measured in methanol and its mixtures with dimethyl sulfoxide (10 to 80% v/v) using sodium methoxide as the base. The experimental dissociation constants have been used to construct the H- acidity function as a function of methoxide concentration and composition of the DMSO-MeOH mixture as well as function of methoxide concentration in methanol. Moreover, with the help of construction of acidity function, the functions have been devised for constant sodium methoxide concentrations (0.025, 0.1, and 0.2 mol 1-1) and changing composition of the DMSO-MeOH mixture.
Synthesis and Evaluation of N-Phenylpyrrolamides as DNA Gyrase B Inhibitors
Durcik, Martina,Tammela, P?ivi,Baran?oková, Michaela,Toma?i?, Tihomir,Ila?, Janez,Kikelj, Danijel,Zidar, Nace
supporting information, p. 186 - 198 (2018/02/06)
ATP-competitive inhibitors of DNA gyrase and topoisomerase IV are among the most interesting classes of antibacterial drugs that are unrepresented in the antibacterial pipeline. We developed 32 new N-phenylpyrrolamides and evaluated them against DNA gyrase and topoisomerase IV from E. coli and Staphylococcus aureus. Antibacterial activities were studied against Gram-positive and Gram-negative bacterial strains. The most potent compound displayed an IC50 of 47 nm against E. coli DNA gyrase, and a minimum inhibitory concentration (MIC) of 12.5 μm against the Gram-positive Enterococcus faecalis. Some compounds displayed good antibacterial activities against an efflux-pump-deficient E. coli strain (MIC=6.25 μm) and against wild-type E. coli in the presence of efflux pump inhibitor PAβN (MIC=3.13 μm). Here we describe new findings regarding the structure–activity relationships of N-phenylpyrrolamide DNA gyrase B inhibitors and investigate the factors that are important for the antibacterial activity of this class of compounds.
N-Phenyl-4,5-dibromopyrrolamides and N-Phenylindolamides as ATP Competitive DNA Gyrase B Inhibitors: Design, Synthesis, and Evaluation
Zidar, Nace,Macut, Helena,Toma?i?, Tihomir,Brvar, Matja?,Montalv?o, Sofia,Tammela, P?ivi,Solmajer, Tom,Peterlin Ma?i?, Lucija,Ila?, Janez,Kikelj, Danijel
supporting information, p. 6179 - 6194 (2015/08/24)
Bacterial DNA gyrase is a well-known and validated target in the design of antibacterial drugs. However, inhibitors of its ATP binding subunit, DNA gyrase B (GyrB), have so far not reached clinical use. In the present study, three different series of N-ph