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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:	BIBFORM076534
Első szerző:	Tevyashova, Anna N.
Cím:	Synthesis and evaluation of biological activity for dual-acting antibiotics on the basis of azithromycin and glycopeptides / Anna N. Tevyashova, Elena N. Bychkova, Alexander M. Korolev, Elena B. Isakova, Elena P. Mirchink, Ilya A. Osterman, Réka Erdei, Zsolt Szücs, Gyula Batta
Dátum:	2019
ISSN:	0960-894X
Megjegyzések:	One of the promising directions of the combined approach is the design of dual-acting antibiotics ? heterodimeric structures on the basis of antimicrobial agents of different classes. In this study a novel series of azithromycin-glycopeptide conjugates were designed and synthesized. The structures of the obtained compounds were confirmed using NMR spectroscopy and mass spectrometry data including MS/MS analysis. All novel hybrid antibiotics were found to be either as active as azithromycin and vancomycin against Gram-positive bacterial strains or have superior activity in comparison with their parent antibiotics. One compound, eremomycin-azithromycin conjugate 16, demonstrated moderate activity against Enterococcus faecium and Enterococcus faecalis strains resistant to vancomycin, and equal to vancomycin's activity for the treatment of mice with Staphylococcus aureus sepsis.
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban Macrolide antibiotics Azithromycin Glycopeptide antibiotics Vancomycin Eremomycin Dual action antibiotics Antibacterial activity Mechanism of action
Megjelenés:	Bioorganic & Medicinal Chemistry Letters. - 29 : 2 (2019), p. 276-280. -
További szerzők:	Bychkova, Elena N. Korolev, Alexander M. Isakova, Elena B. Mirchink, Elena P. Osterman, Ilya A. Erdei Réka Szűcs Zsolt (1991-) (gyógyszerész) Batta Gyula (1953-) (molekula-szerkezet kutató)
Pályázati támogatás:	GINOP-2.3.2-15-2016-00008 GINOP GINOP-2.3.3-15-2016-00004 GINOP
Internet cím:	Szerző által megadott URL DOI Intézményi repozitóriumban (DEA) tárolt változat
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