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Št. zadetkov: 3
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)
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)
Izvirni znanstveni članek
Oznake: covalent inhibitor;MurA;cyclobutenaminone;antibacterial;irreversible;
Drug discovery programs against the antibacterial target UDP-N-acetylglucosamine enolpyruvyl transferase (MurA) have already resulted in covalent inhibitors having small three- and five-membered heterocyclic rings. In the current study, the reactivity of four-membered rings was carefully modulated t ...
Leto: 2020 Vir: Fakulteta za farmacijo (UL FFA)
Št. zadetkov: 3
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