Martina Durcik (Avtor), Päivi Tammela (Avtor), Michaela Barančokova (Avtor), Tihomir Tomašić (Avtor), Janez Ilaš (Avtor), Danijel Kikelj (Avtor), Nace Zidar (Avtor)

Povzetek

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 47micro nm against E.coli DNA gyrase, and a minimum inhibitory concentration (MIC) of 12.5 microm against the Gram-positive Enterococcus faecalis. Some compounds displayed good antibacterial activities against an efflux-pump-deficient E. coli strain (MIC=6.25 microm) and against wild-type E. coli in the presence of efflux pump inhibitor PAbetaN (MIC=3.13 microm). 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.

Ključne besede

DNA gyrase;GyrB;antibacterials;inhibitors;pyrrolamides;

Podatki

Jezik: Angleški jezik
Leto izida:
Tipologija: 1.01 - Izvirni znanstveni članek
Organizacija: UL FFA - Fakulteta za farmacijo
UDK: 543.2/.9.057
COBISS: 4461681 Povezava se bo odprla v novem oknu
ISSN: 1860-7187
Št. ogledov: 1016
Št. prenosov: 662
Ocena: 0 (0 glasov)
Metapodatki: JSON JSON-RDF JSON-LD TURTLE N-TRIPLES XML RDFA MICRODATA DC-XML DC-RDF RDF

Ostali podatki

Sekundarni jezik: Slovenski jezik
Vrsta dela (COBISS): Članek v reviji
Konec prepovedi (OpenAIRE): 2019-01-22
Strani: str. 186-198
Letnik: ǂVol. ǂ13
Zvezek: ǂiss. ǂ2
Čas izdaje: 2018
DOI: 10.1002/cmdc.201700549
ID: 11043211