Pregled bibliografske jedinice broj: 515513
Synthesis, activity and pharmacokinetics of novel antibacterial 15-membered ring macrolones
Synthesis, activity and pharmacokinetics of novel antibacterial 15-membered ring macrolones // European Journal of Medicinal Chemistry, 46 (2011), 8; 3388-3397 doi:10.1016/j.ejmech.2011.05.002 (međunarodna recenzija, članak, znanstveni)
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Naslov
Synthesis, activity and pharmacokinetics of novel antibacterial 15-membered ring macrolones
Autori
Fajdetić, Andreja ; Vinter, Adrijana ; Čipčić Paljetak, Hana ; Padovan, Jasna ; Palej Jakopović, Ivana ; Kapić, Samra ; Alihodžić, Sulejman ; Filić, Darko ; Modrić, Marina ; Košutić-Hulita, Nada ; Antolović, Roberto ; Ivezić Schoenfeld, Zrinka ; Mutak, Stjepan ; Eraković Haber, Vesna ; Spaventi, Radan
Izvornik
European Journal of Medicinal Chemistry (0223-5234) 46
(2011), 8;
3388-3397
Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni
Ključne riječi
makrolide; resistance; antibacterial activity; pharmacokinetics; oral bioavailability
Sažetak
Synthesis, antibacterial activity and pharmacokinetic properties of a novel class of macrolide antibioticsdmacrolonesdderived from azithromycin, comprising oxygen atom(s) in the linker and either free or esterified quinolone 3-carboxylic group, are reported. Selected compounds showed excellent antibacterial potency towards key erythromycin resistant respiratory pathogens. However, the majority of compounds lacked good bioavailability. The isopropyl ester, compound 35, and a macrolone derivative with an elongated linker 29 showed the best oral bioavailability in rats, both accompanied with an excellent overall microbiology profile addressing inducible and constitutive MLSb as well as efflux mediated macrolide resistance in streptococci, while compound 29 is more potent against staphylococci.
Izvorni jezik
Engleski
Znanstvena područja
Kemija, Temeljne medicinske znanosti
POVEZANOST RADA
Ustanove:
Fidelta d.o.o.
Profili:
Ivana Palej Jakopović
(autor)
Marina Modrić
(autor)
Vesna Eraković Haber
(autor)
Sulejman Alihodžić
(autor)
Jasna Padovan
(autor)
Zrinka Ivezić
(autor)
Nada Košutić-Hulita
(autor)
Hana Čipčić Paljetak
(autor)
Samra Kapić
(autor)
Andreja Fajdetić
(autor)
Darko Filić
(autor)
Stjepan Mutak
(autor)
Radan Spaventi
(autor)
Roberto Antolović
(autor)
Adrijana Vinter
(autor)
Citiraj ovu publikaciju:
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