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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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001-es BibID:	BIBFORM076534
035-os BibID:	(WoS)000454616600030 (Scopus)85059218639
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 folyóiratcikk 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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