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001-es BibID:	BIBFORM090862
035-os BibID:	(WoS)000622919300001 (Scopus)85099773383
Első szerző:	Izsépi László
Cím:	Bacterial Cell Wall Analogue Peptides Control the Oligomeric States and Activity of the Glycopeptide Antibiotic Eremomycin : solution NMR and Antimicrobial Studies / László Izsépi, Réka Erdei, Anna N. Tevyashova, Natalia E. Grammatikova, Andrey E. Shchekotikhin, Pál Herczegh, Gyula Batta
Dátum:	2021
ISSN:	1424-8247
Megjegyzések:	For some time, glycopeptide antibiotics have been considered the last line of defense against Methicillin-resistant Staphylococcus aureus (MRSA). However, vancomycin resistance of Gram-positive bacteria is an increasingly emerging worldwide health problem. The mode of action of glycopeptide antibiotics is essentially the binding of peptidoglycan cell-wall fragments terminating in the D-Ala-D-Ala sequence to the carboxylate anion binding pocket of the antibiotic. Dimerization of these antibiotics in aqueous solution was shown to persist and even to enhance the antibacterial effect in a co-operative manner. Some works based on solid state (ss) Nuclear Magnetic Resonance (NMR) studies questioned the presence of dimers under the conditions of ssNMR while in a few cases, higher-order oligomers associated with contiguous back-to-back and face-to-face dimers were observed in the crystal phase. However, it is not proved if such oligomers persist in aqueous solutions. With the aid of 15N-labelled eremomycin using 15N relaxation and diffusion NMR methods, we observed tetramers and octamers when the N-Ac-D-Ala-D-Ala dipeptide was added. To the contrary, the N-Ac-D-Ala or (N-Ac)2-L-Lys-D-Ala-D-Ala tripeptide did not induce higher-order oligomers. These observations are interesting examples of tailored supramolecular self-organization. New antimicrobial tests have also been carried out with these self-assemblies against MRSA and VRE (resistant) strains.
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk glycopeptide resistance eremomycin dimer oligomer N-Ac-D-Ala-D-Ala ligand 15N relaxation diffusion NMR
Megjelenés:	Pharmaceuticals. - 14 : 2 (2021), p. 1-14. -
További szerzők:	Erdei Réka Tevyashova, Anna N. Grammatikova, Natalia E. Shchekotikhin, Andrey E. Herczegh Pál (1947-) (vegyész, antibiotikumkémikus) Batta Gyula (1953-) (molekula-szerkezet kutató)
Pályázati támogatás:	GINOP-2.3.2-15-2016-00008 GINOP GINOP-2.3.3-15-2016-00004 GINOP NKFIH K119509 Egyéb
Internet cím:	Szerző által megadott URL DOI Intézményi repozitóriumban (DEA) tárolt változat
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001-es BibID:	BIBFORM094439
035-os BibID:	(cikkazonosító)379 (WoS)000643364900001 (Scopus)85105365400
Első szerző:	Moiseenko, Elena I.
Cím:	Aminoalkylamides of Eremomycin Exhibit an Improved Antibacterial Activity / Elena I. Moiseenko, Réka Erdei, Natalia E. Grammatikova, Elena P. Mirchink, Elena B. Isakova, Eleonora R. Pereverzeva, Gyula Batta, Andrey E. Shchekotikhin
Dátum:	2021
ISSN:	1424-8247
Megjegyzések:	After decades, the glycopeptide vancomycin is still the preferred antibiotic against resistant strains of Gram-positive bacteria. Although its clinical use is strictly regulated, the gradual spread of vancomycin-resistant bacteria, such as glycopeptide-resistant and glycopeptide-intermediate Staphylococcus aureus and vancomycin-resistant Enterococcus spp., is a serious health problem. Based on the literature data and previous studies, our main goal was to assess the antimicrobial potential and to study the structure-activity relationship of new eremomycin aminoalkylamides. We designed and synthesized a series of new eremomycin amides in which eremomycin is conjugated with a hydrophobic arylalkyl group via an alkylenediamine spacer, and tested their antibacterial activities on a panel of Gram-positive strains that were sensitive and resistant to a "gold-standard" vancomycin. Based on the data obtained, the structure-activity relationships were investigated, and a lead compound was selected for in-depth testing. Research carried out using an in vivo model of staphylococcus sepsis, acute toxicity studies, and the estimated therapeutic index also showed the advantage of the selected eremomycin amide derivative in particular, as well as the chosen direction in general.
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk glycopeptide antibiotics vancomycin eremomycin semisynthetic antibiotics Gram-positive antibacterial activity
Megjelenés:	Pharmaceuticals. - 14 : 4 (2021), p. 1-19. -
További szerzők:	Erdei Réka Grammatikova, Natalia E. Mirchink, Elena P. Isakova, Elena B. Pereverzeva, Eleonora R. Batta Gyula (1953-) (molekula-szerkezet kutató) Shchekotikhin, Andrey E.
Internet cím:	Szerző által megadott URL DOI Intézményi repozitóriumban (DEA) tárolt változat
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