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

Povzetek

Development of novel DNA gyrase B inhibitors is an important field of antibacterial drug discovery whose aim is to introduce a more effective representative of this mechanistic class into the clinic. In the present study, two new series of Escherichia coli DNA gyrase inhibitors bearing the 4,5-dibromopyrrolamide moiety have been designed and synthesized. 4,5,6,7-Tetrahydrobenzo[1,2-d]thiazole-2,6-diamine derivatives inhibited E. coli DNA gyrase in the submicromolar to low micromolar range (IC50 values between 0.891 and 10.4 microM). Their ''ring-opened'' analogues, based on the 2-(2-aminothiazol-4-yl)acetic acid scaffold, displayed weaker DNA gyrase inhibition with IC50 values between 15.9 and 169 microM. Molecular docking experiments were conducted to study the binding modes of inhibitors.

Ključne besede

antibacterial;DNA gyrase;docking;inhibitor;thiazole;

Podatki

Jezik: Angleški jezik
Leto izida:
Tipologija: 1.01 - Izvirni znanstveni članek
Organizacija: UL FFA - Fakulteta za farmacijo
UDK: 543:615.015.8
COBISS: 4240753 Povezava se bo odprla v novem oknu
ISSN: 0968-0896
Št. ogledov: 1140
Št. prenosov: 790
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): Znanstveno delo
Konec prepovedi (OpenAIRE): 2019-01-01
Strani: str. 338-349
Letnik: ǂVol. ǂ25
Zvezek: ǂiss. ǂ1
Čas izdaje: 2017
DOI: 10.1016/j.bmc.2016.10.038
ID: 11043210