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Pregled bibliografske jedinice broj: 721681

N'-substituted-2'-O, 3'-N-carbonimidoyl bridged macrolides : novel anti-inflammatory macrolides without antimicrobial activity


Bosnar, Martina; Kragol, Goran; Koštrun, Sanja; Vujasinović, Ines; Bošnjak, Berislav; Mihaljević-Bencetić, Vlatka; Ištuk-Marušić, Zorica; Kapić, Samra; Hrvačić, Boška; Brajša, Karmen et al.
N'-substituted-2'-O, 3'-N-carbonimidoyl bridged macrolides : novel anti-inflammatory macrolides without antimicrobial activity // Journal of medicinal chemistry, 55 (2012), 13; 6111-6123 doi:10.1021/jm300356u (međunarodna recenzija, članak, znanstveni)


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Naslov
N'-substituted-2'-O, 3'-N-carbonimidoyl bridged macrolides : novel anti-inflammatory macrolides without antimicrobial activity

Autori
Bosnar, Martina ; Kragol, Goran ; Koštrun, Sanja ; Vujasinović, Ines ; Bošnjak, Berislav ; Mihaljević-Bencetić, Vlatka ; Ištuk-Marušić, Zorica ; Kapić, Samra ; Hrvačić, Boška ; Brajša, Karmen ; Tavčar, Branka ; Jelić, Dubravko ; Glojnarić, Ines ; Verbanac, Donatella ; Čulić, Ognjen ; Padovan, Jasna ; Alihodžić, Sulejman ; Haber-Eraković, Vesna ; Spaventi, Radan

Izvornik
Journal of medicinal chemistry (0022-2623) 55 (2012), 13; 6111-6123

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
antininflammatory; macrolides

Sažetak
Macrolide antibiotics, like erythromycin, clarithromycin, and azithromycin, possess anti- inflammatory properties. These properties are considered fundamental to the efficacy of these three macrolides in the treatment of chronic inflammatory diseases like diffuse panbronchiolitis and cystic fibrosis. However, long-term treatment with macrolide antibiotics presents a considerable risk for promotion of bacterial resistance. We have examined antibacterial and anti-inflammatory effects of a novel macrolide class: N'-substituted 2'-O, 3'-N-carbonimidoyl bridged erythromycin-derived 14- and 15-membered macrolides. A small focused library was prepared, and compounds without antimicrobial activity, which inhibited IL-6 production, were selected. Data analysis led to a statistical model that could be used for the design of novel anti-inflammatory macrolides. The most promising compound from this library retained the anti-inflammatory activity observed with azithromycin in lipopolysaccharide-induced pulmonary neutrophilia in vivo. Importantly, this study strongly suggests that antimicrobial and anti- inflammatory activities of macrolides are independent and can be separated, which raises development plausibility of novel anti- inflammatory therapeutics

Izvorni jezik
Engleski

Znanstvena područja
Farmacija



POVEZANOST RADA


Ustanove:
Pliva-Istraživački institut

Citiraj ovu publikaciju

Bosnar, Martina; Kragol, Goran; Koštrun, Sanja; Vujasinović, Ines; Bošnjak, Berislav; Mihaljević-Bencetić, Vlatka; Ištuk-Marušić, Zorica; Kapić, Samra; Hrvačić, Boška; Brajša, Karmen et al.
N'-substituted-2'-O, 3'-N-carbonimidoyl bridged macrolides : novel anti-inflammatory macrolides without antimicrobial activity // Journal of medicinal chemistry, 55 (2012), 13; 6111-6123 doi:10.1021/jm300356u (međunarodna recenzija, članak, znanstveni)
Bosnar, M., Kragol, G., Koštrun, S., Vujasinović, I., Bošnjak, B., Mihaljević-Bencetić, V., Ištuk-Marušić, Z., Kapić, S., Hrvačić, B. & Brajša, K. (2012) N'-substituted-2'-O, 3'-N-carbonimidoyl bridged macrolides : novel anti-inflammatory macrolides without antimicrobial activity. Journal of medicinal chemistry, 55 (13), 6111-6123 doi:10.1021/jm300356u.
@article{article, year = {2012}, pages = {6111-6123}, DOI = {10.1021/jm300356u}, keywords = {antininflammatory, macrolides}, journal = {Journal of medicinal chemistry}, doi = {10.1021/jm300356u}, volume = {55}, number = {13}, issn = {0022-2623}, title = {N'-substituted-2'-O, 3'-N-carbonimidoyl bridged macrolides : novel anti-inflammatory macrolides without antimicrobial activity}, keyword = {antininflammatory, macrolides} }
@article{article, year = {2012}, pages = {6111-6123}, DOI = {10.1021/jm300356u}, keywords = {antininflammatory, macrolides}, journal = {Journal of medicinal chemistry}, doi = {10.1021/jm300356u}, volume = {55}, number = {13}, issn = {0022-2623}, title = {N'-substituted-2'-O, 3'-N-carbonimidoyl bridged macrolides : novel anti-inflammatory macrolides without antimicrobial activity}, keyword = {antininflammatory, macrolides} }

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


Uključenost u ostale bibliografske baze podataka:


  • MEDLINE
  • British Library Serials


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