19788-77-3Relevant articles and documents
Macrolactonolides: A novel class of anti-inflammatory compounds
Toma?kovi?, Linda,Komac, Marijana,Makaruha Stegi?, Oresta,Muni?, Vesna,Rali?, Jovica,Stani?, Barbara,Banjanac, Mihailo,Markovi?, Stribor,Hrva?i?, Bo?ka,?ip?i? Paljetak, Hana,Padovan, Jasna,Glojnari?, Ines,Erakovi? Haber, Vesna,Mesi?, Milan,Mer?ep, Mladen
, p. 321 - 332 (2013)
A new concept in design of safe glucocorticoid therapy was introduced by conjugating potent glucocorticoid steroids with macrolides (macrolactonolides). These compounds were synthesized from various steroid 17β-carboxylic acids and 9a-N-(3-aminoalkyl) derivatives of 9-deokso-9a-aza-9a-homoeritromicin A and 3-descladinosyl-9-deokso-9a-aza-9a-homoeritromicin A using stable alkyl chain. Combining property of macrolides to preferentially accumulate in immune cells, especially in phagocyte cells, with anti-inflammatory activity of classic steroids, we designed molecules which showed good anti-inflammatory activity in ovalbumin (OVA) induced asthma in rats. The synthesis, in vitro and in vivo anti-inflammatory activity of this novel class of compounds are described.