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Pregled bibliografske jedinice broj: 1085455

Discovery of macrozones, new antimicrobial thiosemicarbazone-based azithromycin conjugates: design, synthesis and in vitro biological evaluation


Grgičević, Ivan; Mikulandra, Ivana; Bukvić, Mirjana; Banjanac, Mihailo, Radovanović, Vedrana; Habinovec, Iva; Bertoša, Branimir; Novak, Predrag
Discovery of macrozones, new antimicrobial thiosemicarbazone-based azithromycin conjugates: design, synthesis and in vitro biological evaluation // International journal of antimicrobial agents, 56 (2020), 106147, 5 (međunarodna recenzija, kratko priopcenje, znanstveni)


CROSBI ID: 1085455 Za ispravke kontaktirajte CROSBI podršku putem web obrasca

Naslov
Discovery of macrozones, new antimicrobial thiosemicarbazone-based azithromycin conjugates: design, synthesis and in vitro biological evaluation

Autori
Grgičević, Ivan ; Mikulandra, Ivana ; Bukvić, Mirjana ; Banjanac, Mihailo, Radovanović, Vedrana ; Habinovec, Iva ; Bertoša, Branimir ; Novak, Predrag

Izvornik
International journal of antimicrobial agents (0924-8579) 56 (2020); 106147, 5

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, kratko priopcenje, znanstveni

Ključne riječi
macrozones, azithromycin, thiosemicarbazones, in vitro evaluation, antibacterials, resistance

Sažetak
Increasing bacterial resistance to existing antibiotics presents a serious threat to human health, and new antibacterial agents are desperately needed. Unfortunately, the number of newly marketed antibiotics has decreased dramatically in recent years. Withdrawal of the macrolide antibiotic telithromycin and inability of solithromycin to gain marketing approval have prompted our efforts to search for new anti-infective macrolide compounds. Here we present the design, synthesis and biological evaluation of a novel hybrid class of azithromycin conjugates, the macrozones. Evaluation of prepared compounds against a panel of pathogenic bacteria revealed that these molecules showed excellent activities against susceptible Streptococcus pneumoniae, Streptococcus pyogenes and Enterococcus faecalis strains comparable with or better than azithromycin. Furthermore, prepared macrozones exhibited excellent activity against efflux resistant S.pneumoniae, which was 32 times better than that of azithromycin, and very good activity against efflux resistant Staphylococcus aureus strain against which azithromycin is inactive. The results described here can serve as a good basis to guide further activities directed toward the discovery of more potent macrolide anti-infectives.

Izvorni jezik
Engleski

Znanstvena područja
Kemija



POVEZANOST RADA


Projekti:
HRZZ-IP-2018-01-8098 - Makrozoni, novi konjugati makrolidnih antibiotika: Dizajn, priprava i interakcije (Makrozoni/Macrozones) (Novak, Predrag, HRZZ - 2018-01) ( POIROT)

Ustanove:
Prirodoslovno-matematički fakultet, Zagreb,
Fidelta d.o.o.


Citiraj ovu publikaciju

Grgičević, Ivan; Mikulandra, Ivana; Bukvić, Mirjana; Banjanac, Mihailo, Radovanović, Vedrana; Habinovec, Iva; Bertoša, Branimir; Novak, Predrag
Discovery of macrozones, new antimicrobial thiosemicarbazone-based azithromycin conjugates: design, synthesis and in vitro biological evaluation // International journal of antimicrobial agents, 56 (2020), 106147, 5 (međunarodna recenzija, kratko priopcenje, znanstveni)
Grgičević, I., Mikulandra, I., Bukvić, M., Banjanac, Mihailo, Radovanović, Vedrana, Habinovec, I., Bertoša, B. & Novak, P. (2020) Discovery of macrozones, new antimicrobial thiosemicarbazone-based azithromycin conjugates: design, synthesis and in vitro biological evaluation. International journal of antimicrobial agents, 56, 106147, 5.
@article{article, year = {2020}, pages = {5}, chapter = {106147}, keywords = {macrozones, azithromycin, thiosemicarbazones, in vitro evaluation, antibacterials, resistance}, journal = {International journal of antimicrobial agents}, volume = {56}, issn = {0924-8579}, title = {Discovery of macrozones, new antimicrobial thiosemicarbazone-based azithromycin conjugates: design, synthesis and in vitro biological evaluation}, keyword = {macrozones, azithromycin, thiosemicarbazones, in vitro evaluation, antibacterials, resistance}, chapternumber = {106147} }
@article{article, year = {2020}, pages = {5}, chapter = {106147}, keywords = {macrozones, azithromycin, thiosemicarbazones, in vitro evaluation, antibacterials, resistance}, journal = {International journal of antimicrobial agents}, volume = {56}, issn = {0924-8579}, title = {Discovery of macrozones, new antimicrobial thiosemicarbazone-based azithromycin conjugates: design, synthesis and in vitro biological evaluation}, keyword = {macrozones, azithromycin, thiosemicarbazones, in vitro evaluation, antibacterials, resistance}, chapternumber = {106147} }

Časopis indeksira:


  • Current Contents Connect (CCC)
  • Web of Science Core Collection (WoSCC)
    • Science Citation Index Expanded (SCI-EXP)
    • SCI-EXP, SSCI i/ili A&HCI
  • Scopus
  • MEDLINE





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