izpis_h1_title_alt

Novel 2-thioxothiazolidin-4-one inhibitors of bacterial MurD ligase targeting d-Glu- and diphosphate-binding site
Tomašič, Tihomir (Avtor), Kovač, Andreja (Avtor), Simčič, Mihael (Avtor), Blanot, Didier (Avtor), Golič Grdadolnik, Simona (Avtor), Gobec, Stanislav (Avtor), Kikelj, Danijel (Avtor), Peterlin-Mašič, Lucija (Avtor)

URLURL - Predstavitvena datoteka, za dostop obiščite http://www.sciencedirect.com/science?_ob=PublicationURL&_tockey=%23TOC%236135%239999%23999999999%2399999%23FLA%23&_cdi=6135&_pubType=J&_auth=y&_acct=C000033658&_version=1&_urlVersion=0&_userid=4776866&md5=b8e2545f2e5ef25705d793d113fd023f Novo okno

Izvleček
Mur ligases are involved in cytoplasmic steps of bacterial peptidoglycan biosynthesis and are viable targets for antibacterial drug discovery. We have designed and synthesized a focused chemical library of compounds combining the glutamic acid moiety and the 2-thioxothiazolidin-4-one, thiazolidine-2,4-dione, 2-iminothiazolidin-4-one or imidazolidine-2,4-dione ring connected by a benzylidene group. These compounds were designed to targetthe d-Glu- and the diphosphate-binding pockets of the MurD active site and were evaluated for inhibition of MurD ligase from Escherichia coli. The most potent compounds (R)-9 and (S)-9 inhibited MurD with IC50 values of 45 [micro]M and 10 [microm]M, respectively. The specific binding mode of (R)-9 in MurD active site was established by high-resolution NMR spectroscopy.

Jezik:Angleški jezik
Ključne besede:Mur Ligaze, protivnetna zdravila, protein NMR, inihbitorji
Vrsta gradiva:Delo ni kategorizirano (r6)
Tipologija:1.01 - Izvirni znanstveni članek
Organizacija:FFA - Fakulteta za farmacijo
Leto izida:2011
Št. strani:str. 3964-3975
Številčenje:Vol. 46, issue 9
UDK:542:615.2
ISSN pri članku:0223-5234
DOI:10.1016/j.ejmech.2011.05.070 Povezava se odpre v novem oknu
COBISS.SI-ID:3030897 Povezava se odpre v novem oknu
Število ogledov:383
Število prenosov:278
Metapodatki:XML RDF-CHPDL DC-XML DC-RDF
 
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Gradivo je del revije

Naslov:European journal of medicinal chemistry
Skrajšan naslov:Eur. j. med. chem.
Založnik:Elsevier
ISSN:0223-5234
COBISS.SI-ID:25429760 Novo okno

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