Št. zadetkov: 16
Magistrsko delo
Oznake:
protibakterijske učinkovine;DNA giraza B;N-fenilpirolamid;zaviralci giraz;sintezni postopki;
Načrtovanje in sinteza novih N-fenilpirolamidnih zaviralcev DNA-giraze B
Leto:
2017
Vir:
Fakulteta za farmacijo (UL FFA)
Magistrsko delo
Oznake:
konjugat;ciprofloksacin;benzotiazolpirolamid;dvojni zaviralec;DNA-giraza A/DNA-giraza B;protibakterijska učinkovina;
V boju proti bakterijski odpornosti obetavno strategijo predstavlja razvoj večtarčnih zaviralcev bakterijskih encimov. Z omenjeno strategijo lahko zmanjšamo sposobnost bakterij za razvoj tarčne odpornosti proti protibakterijskim spojinam. Ena od privlačnih tarč za razvoj protibakterijskih spojin je ...
Leto:
2021
Vir:
Fakulteta za farmacijo (UL FFA)
Doktorska disertacija
Oznake:
Benzotiazol;DNA-giraza;topoizomeraza IV;dvojni zaviralci;protibakterijsko delovanje;bakterijska odpornost;
Bakterijska encima DNA-giraza in topoizomeraza IV sta validirani tarči za odkrivanje novih protibakterijskih učinkovin. Zaradi svoje strukturne podobnosti omogočata načrtovanje spojin, ki lahko sočasno zavirajo oba encima, take spojine pa so lahko uspešnejše v boju proti bakterijski odpornosti, ki s ...
Leto:
2023
Vir:
Fakulteta za farmacijo (UL FFA)
Izvirni znanstveni članek
Oznake:
bisphenol sulfates;sulfation kinetics;sulfate estrogenic activity;sulfate stability;
Bisphenols are endocrine-disrupting chemicals ubiquitously present in the environment, with the consequent exposure to humans. In humans, bisphenols are metabolized to glucuronide and sulfate conjugates. Recent studies indicate that sulfation represents an important bisphenol metabolic pathway for t ...
Leto:
2022
Vir:
Fakulteta za farmacijo (UL FFA)
Izvirni znanstveni članek
Oznake:
bisphenols;concentration addition;environmental water;estrogenic activity;hormones;mixtures;
Endocrine disrupting chemicals such as natural and synthetic steroid hormones and bisphenols are among the most important pollutants in the aquatic environment. We performed an environmental chemical analysis of five Slovenian water samples, two rivers, one groundwater, and the influent and effluent ...
Leto:
2023
Vir:
Fakulteta za farmacijo (UL FFA)
Izvirni znanstveni članek
Oznake:
zaviralci;benzotiazol;alosterija;allosteric;Hsp90;benzothiazole;cancer;inhibitor;cancer therapy;
Heat shock protein 90 (Hsp90) is a chaperone responsible for the maturation of many cancer-related proteins, and is therefore an important target for the design of new anticancer agents. Several Hsp90 N-terminal domain inhibitors have been evaluated in clinical trials, but none have been approved as ...
Leto:
2021
Vir:
Fakulteta za farmacijo (UL FFA)
Izvirni znanstveni članek
Oznake:
DNA gyrase;GyrB;antibacterials;inhibitors;pyrrolamides;
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 Staph ...
Leto:
2018
Vir:
Fakulteta za farmacijo (UL FFA)
Izvirni znanstveni članek
Oznake:
napetostno odvisni natrijev kanal;Nav kanal;Nav1.3;zaviralci;arilsulfonamid;acilsulfonamid;Voltage-gated sodium channel;Nav channel;inhibitor;arylsulfonamide;acylsulfonamide;
Voltage-gated sodium channels (Navs) play an essential role in neurotransmission, and their dysfunction is often a cause of various neurological disorders. The Nav1.3 isoform is found in the CNS and upregulated after injury in the periphery, but its role in human physiology has not yet been fully el ...
Leto:
2023
Vir:
Fakulteta za farmacijo (UL FFA)
Izvirni znanstveni članek
Oznake:
luciferin;sinteza spojin;bioaktivne spojine;benzo[d]thiazol;medicinal chemistry;
Benzo[d]thiazole is widely used in synthetic and medicinal chemistry, and it is a component of many compounds and drugs that have several different bioactivities. Herein, we describe an elegant pathway for synthesis of methyl 4- and 5-hydroxy-2-amino-benzo[d]thiazole-6-carboxylates as building block ...
Leto:
2020
Vir:
Fakulteta za farmacijo (UL FFA)
Izvirni znanstveni članek
Oznake:
zaviralci;molekularna dinamika;zdravljenje raka;virtualno rešetanje;farmakofori;allosteric;cancer;Hsp90;inhibitor;molecular dynamics;pharmacophores;virtual screening;
Hsp90 C-terminal domain (CTD) inhibitors are promising novel agents for cancer treatment, as they do not induce the heat shock response associated with Hsp90 N-terminal inhibitors. One challenge associated with CTD inhibitors is the lack of a co-crystallized complex, requiring the use of predicted a ...
Leto:
2020
Vir:
Fakulteta za farmacijo (UL FFA)