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N'-substituted-2'-O, 3'-N-carbonimidoyl bridged macrolides : novel anti-inflammatory macrolides without antimicrobial activity (CROSBI ID 209960)

Prilog u časopisu | izvorni znanstveni rad | međunarodna recenzija

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

Podaci o odgovornosti

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

engleski

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

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

antininflammatory; macrolides

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Podaci o izdanju

55 (13)

2012.

6111-6123

objavljeno

0022-2623

10.1021/jm300356u

Povezanost rada

Farmacija

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