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Structure-activity relationships of new cyanothiophene inhibitors of the essential peptidoglycan biosynthesis enzyme MurF
Hrast, Martina (Avtor), Turk, Samo (Avtor), Sosič, Izidor (Avtor), Knez, Damijan (Avtor), Randall, Christopher P. (Avtor), Barreteau, Hélène (Avtor), Contreras-Martel, Carlos (Avtor), Dessen, Andréa (Avtor), O'Neill, Alex J. (Avtor), Mengin-Lecreulx, Dominique (Avtor), Blanot, Didier (Avtor), Gobec, Stanislav (Avtor)

URLURL - Predstavitvena datoteka, za dostop obiščite http://www.sciencedirect.com/science/article/pii/S0223523413003139 Povezava se odpre v novem oknu

Izvleček
Peptidoglycan is an essential component of the bacterial cell wall, and enzymes involved in its biosynthesis represent validated targets for antibacterial drug discovery. MurF catalyzes the final intracellular peptidoglycan biosynthesis step: the addition of d-Ala-d-Ala to the nucleotide precursor UDP-MurNAc-l-Ala-Ž-d-Glu-meso-DAP (or l-Lys). As MurF has no human counterpart, it represents an attractive target for the development of new antibacterial drugs. Using recently published cyanothiophene inhibitors of MurF from Streptococcus pneumoniae as a starting point, we designed and synthesized a series of structurally related derivatives and investigated their inhibition of MurF enzymes from different bacterial species. Systematic structural modifications of the parent compounds resulted in a series of nanomolar inhibitors of MurF from S. pneumoniae and micromolar inhibitors of MurF from Escherichia coli and Staphylococcus aureus. Some of the inhibitors also show antibacterial activity against S. pneumoniae R6. These findings, together with two new co-crystal structures, represent an excellent starting point for further optimization towards effective novel antibacterials.

Jezik:Angleški jezik
Ključne besede:MurF inhibitorji, protivnetne učinkovine, kristalne strukture, Mur ligaze
Vrsta gradiva:Delo ni kategorizirano (r6)
Tipologija:1.01 - Izvirni znanstveni članek
Organizacija:FFA - Fakulteta za farmacijo
Leto izida:2013
Št. strani:str. 32-45
Številčenje:Vol. 66
UDK:548.3+615.2
ISSN pri članku:0223-5234
DOI:10.1016/j.ejmech.2013.05.013 Povezava se odpre v novem oknu
COBISS.SI-ID:3452785 Povezava se odpre v novem oknu
Število ogledov:470
Število prenosov:219
Metapodatki:XML RDF-CHPDL DC-XML DC-RDF
 
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Naslov:European journal of medicinal chemistry
Skrajšan naslov:Eur. j. med. chem.
Založnik:Elsevier
ISSN:0223-5234
COBISS.SI-ID:25429760 Povezava se odpre v novem oknu

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