Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Andrej, Prezelj"'
Publikováno v:
SLAS Discovery. 14:142-150
Cytotoxicity screening of new chemical entities in antibacterial drug discovery discerns between cytotoxic and antimicrobial activity, thus providing predictive evidence for selective toxicity. The objective of this study was to evaluate 3 cytotoxici
Publikováno v:
Antimicrobial Agents and Chemotherapy. 53:505-511
LK-157 is a novel tricyclic carbapenem with potent activity against class A and class C β-lactamases. When tested against the purified TEM-1 and SHV-1 enzymes, LK-157 exhibited 50% inhibitory concentrations (IC 50 s) in the ranges of the clavulanic
Publikováno v:
Current Pharmaceutical Design. 13:2283-2309
The widespread emergence of pathogenic bacterial strains with resistance to antibiotics is becoming a serious threat to public health. Continuous development of novel antibacterials therefore remains one of the biggest challenges to science and unmet
Publikováno v:
Current Pharmaceutical Design. 13:287-312
The drawbacks and limitations of existing anticoagulant therapy which may result in serious adverse effects and a high mortality rate, have given rise to many anticoagulant development programmes in the last decade, focusing mainly at development of
Autor:
Mojca Stegnar, Sebastjan Reven, Danijel Kikelj, Andrej Prezelj, Andreja Kranjc, Lucija Peterlin Mašič, Klemen Mikic
Publikováno v:
European Journal of Medicinal Chemistry. 40:782-791
The design, synthesis and biological activity of new thrombin inhibitors with a pyridinone or pyrazinone core and different heterobicyclic P1 arginine side-chain mimetics are described. The arginine side-chain mimetics used in this study are (±)-4,5
Publikováno v:
The Journal of pharmacy and pharmacology. 61(9)
LK-157 is a novel 10-ethylidene tricyclic carbapenem that resembles the structure of the broad-spectrum antibiotic sanfetrinem and acts as a potent inactivator of beta-lactamases of classes A, C and D. LK-157 is a highly soluble but poorly permeable
Publikováno v:
Chemico-biological interactions. 178(1-3)
Bacterial beta-ketoacyl-[acyl carrier protein] (beta-ketoacyl-ACP) reductase (FabG) is a highly conserved and ubiquitously expressed enzyme of the fatty-acid biosynthetic pathway of prokaryotic organisms that catalyzes NADPH-dependent reduction of be
Autor:
Darko Kocjan, Miha Andrejašič, Tom Solmajer, Tomaz Mesar, Andrej Kocijan, Petra Stefanic Anderluh, Dušan Turk, Mateja Vilar, Lovro Selic, Tadeja Prevec, Anton Copar, Andrej Prezelj, Gregor Vilfan, Uroš Urleb, Marko Oblak, Lars Hesse, Ivan Plantan
Publikováno v:
Journal of medicinal chemistry. 50(17)
A wide variety of pathogens have acquired antimicrobial resistance as an inevitable evolutionary response to the extensive use of antibacterial agents. In particular, one of the most widely used antibiotic structural classes is the beta-lactams, in w
Publikováno v:
Zeitschrift fur Naturforschung. C, Journal of biosciences. 59(11-12)
Several novel thiol-reactive clenbuterol analogues were coupled in high yield with bovine serum albumin (BSA). After labelling of unreacted cysteines with maleimide spin label (MiSL), the yield of the coupling reaction was determined by electron para
Publikováno v:
Die Pharmazie. 59(10)
New inhibitors of serine proteases with azaphenylalanine scaffold were synthesized and their activity was evaluated in vitro. We studied the effect of different substituents in the part of a molecule that binds in the distal pocket of the thrombin ac