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Št. zadetkov: 7
Načrtovanje in sinteza dipeptidnih zaviralcev imunoproteasoma
Katarina Grabrijan, Aleš Obreza, Marko Jukič
Magistrsko delo
Oznake: ubikvitin;imunoproteasom;beta5i-podenota;dipeptidni zaviralci;1,3,4-oksatiazol-2-on;
Načrtovanje in sinteza dipeptidnih zaviralcev imunoproteasoma
Leto: 2017 Vir: Fakulteta za farmacijo (UL FFA)
Synthesis of 3-amino-4-substituted monocyclic ß-lactams - important structural motifs in medicinal chemistry
Katarina Grabrijan, Nika Strašek, Stanislav Gobec
Izvirni znanstveni članek
Oznake: monociklični ß-laktam;Staudingerjeva [2+2] ciklokondenzacija;cerijev amonijev nitrat;hidrazin hidrat;3-amino-4-substituiran azetidin-2-on;inhibitorna aktivnost;monocyclic ß-lactam;Staudinger [2+2] cyclocondensation;cerium ammonium nitrate;hydrazine hydrate;3-amino-4-substituted azetidin-2-one;inhibitory activities;
Monocyclic ß-lactams (azetidin-2-ones) exhibit a wide range of biological activities, the most important of which are antibacterial, anticancer, and cholesterol absorption inhibitory activities. The synthesis of decorated monocyclic ß-lactams is challenging because their ring is highly constrained a ...
Leto: 2022 Vir: Fakulteta za farmacijo (UL FFA)
Načrtovanje, sinteza in vrednotenje novih kovalentnih zaviralcev encimov MurA in penicilin vezočih proteinov
Katarina Grabrijan, Stanislav Gobec, Martina Hrast
Doktorska disertacija
Oznake: penicilin vezoči proteini;MurA;kovalentni zaviralci;monociklični β-laktami;kloracetamidi;
Osredotočili smo se na kovalentne zaviralce encimov, ki sodelujejo v sintezi bakterijskega peptidoglikana. Penicilin vezoči proteini (PBP) sodelujejo v zadnji stopnji sinteze bakterijske celične stene in katalizirajo prečno premreženje peptidoglikana. UDP-N-acetilglukozamin enolpiruvil transferaza ( ...
Leto: 2023 Vir: Fakulteta za farmacijo (UL FFA)
Fragment-sized thiazoles in fragment-based drug discovery campaigns
Matic Proj, Martina Hrast, Damijan Knez, Krištof Bozovičar, Katarina Grabrijan, Anže Meden, Stanislav Gobec, Rok Frlan
Izvirni znanstveni članek
Oznake: thiazoles;hit profiling;promiscuous compounds;frequent hitters;privileged scaffolds;fragments;
Thiazoles exhibit a wide range of biological activities and therefore represent useful and attractive building blocks. To evaluate their usefulness and pinpoint their liabilities in fragment screening campaigns, we assembled a focused library of 49 fragment-sized thiazoles and thiadiazoles with vari ...
Leto: 2022 Vir: Fakulteta za farmacijo (UL FFA)
Synthesis and biochemical evaluation of new 3-amido-4-substituted monocyclic ß-lactams as inhibitors of penicillin-binding protein(s)
Katarina Grabrijan, Nika Strašek, Alen Krajnc, Krištof Bozovičar, Damijan Knez, Matic Proj, Irena Zdovc, Izidor Sosič, Martina Hrast, Stanislav Gobec
Izvirni znanstveni članek
Oznake: antibacterial agents;monocyclic-β-lactams;penicillin-binding proteins;covalent inhibitors;transpeptidase;
In the final phases of bacterial cell wall synthesis, penicillin-binding proteins (PBPs) catalyze the cross-linking of peptidoglycan. For many decades, effective and non-toxic β-lactam antibiotics have been successfully used as mimetics of the d-Ala-d-Ala moiety of the natural substrate and employed ...
Leto: 2024 Vir: Fakulteta za farmacijo (UL FFA)
Covalent inhibitors of bacterial peptidoglycan biosynthesis enzyme MurA with chloroacetamide warhead
Katarina Grabrijan, Martina Hrast, Matic Proj, Ana Dolšak, Irena Zdovc, Tímea Imre, László Petri, Péter Ábrányi-Balogh, György Keserü M., Stanislav Gobec
Izvirni znanstveni članek
Oznake: antibakterijska sredstva;UDP-N-acetilglukozamin enolpiruvil transferaza;tiolna reaktivnost;antibacterial agents;UDP-N-Acetylglucosamine enolpyruvyl transferase;thiol reactivity;
MurA (UDP-N-acetylglucosamine enolpyruvyl transferase) catalyzes the first committed step in the cytoplasmic part of peptidoglycan biosynthesis and is a validated target enzyme for antibacterial drug discovery; the inhibitor fosfomycin has been used clinically for decades. Like fosfomycin, most MurA ...
Leto: 2022 Vir: Fakulteta za farmacijo (UL FFA)
Next-generation heterocyclic electrophiles as small-molecule covalent MurA inhibitors
Péter Ábrányi-Balogh, Aaron Keeley, György G. Ferenczy, László Petri, Tímea Imre, Katarina Grabrijan, Martina Hrast, Damijan Knez, Janez Ilaš, Stanislav Gobec, György Keserü M.
Izvirni znanstveni članek
Oznake: kovalentni inhibitor;heterociklični elektrofili;označevanje cisteina;kvaternizacija;MurA;covalent inhibitor;heterocyclic electrophiles;cysteine labelling;quaternization;
Heterocyclic electrophiles as small covalent fragments showed promising inhibitory activity on the antibacterial target MurA (UDP-N-acetylglucosamine 1-carboxyvinyltransferase, EC:2.5.1.7). Here, we report the second generation of heterocyclic electrophiles: the quaternized analogue of the heterocyc ...
Leto: 2022 Vir: Fakulteta za farmacijo (UL FFA)
Št. zadetkov: 7
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