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Synthesis, activity and pharmacokinetics of novel antibacterial 15-membered ring macrolones


Fajdetić, Andreja; Vinter, Adrijana; Čipčić Paljetak, Hana; Padovan, Jasna; Palej Jakopović, Ivana; Kapić, Samra; Alihodžić, Sulejman; Filić, Darko; Modrić, Marina; Košutić-Hulita, Nada et al.
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)


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

Citiraj ovu publikaciju

Fajdetić, Andreja; Vinter, Adrijana; Čipčić Paljetak, Hana; Padovan, Jasna; Palej Jakopović, Ivana; Kapić, Samra; Alihodžić, Sulejman; Filić, Darko; Modrić, Marina; Košutić-Hulita, Nada et al.
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)
Fajdetić, A., Vinter, A., Čipčić Paljetak, H., Padovan, J., Palej Jakopović, I., Kapić, S., Alihodžić, S., Filić, D., Modrić, M. & Košutić-Hulita, N. (2011) Synthesis, activity and pharmacokinetics of novel antibacterial 15-membered ring macrolones. European Journal of Medicinal Chemistry, 46 (8), 3388-3397 doi:10.1016/j.ejmech.2011.05.002.
@article{article, year = {2011}, pages = {3388-3397}, DOI = {10.1016/j.ejmech.2011.05.002}, keywords = {makrolide, resistance, antibacterial activity, pharmacokinetics, oral bioavailability}, journal = {European Journal of Medicinal Chemistry}, doi = {10.1016/j.ejmech.2011.05.002}, volume = {46}, number = {8}, issn = {0223-5234}, title = {Synthesis, activity and pharmacokinetics of novel antibacterial 15-membered ring macrolones}, keyword = {makrolide, resistance, antibacterial activity, pharmacokinetics, oral bioavailability} }

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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