engleski

Sterolides:design, synthesis and biological evaluation

Although inhaled steroids are the most effective therapy known for asthma, their use over long periods is associated by a number of severe side effects. Several strategies have been employed in development of "safer" anti-inflammatory steroids. We used a novel "sterolide" concept (steroid-macrolide conjugates1-3) where we combined property of macrolides to preferentially accumulate in immune cells, especially in phagocyte cells (peripheral blood mononuclear cells, peritoneal and alveolar macrophages) with potent anti-inflammatory activity of classic steroids. Such sterolide molecules show excellent anti-inflammatory activity in several animal models with little or no systemic effects otherwise seen with standard steroids. Lead molecule is currently in the late preclinical development stage.

sterolides; antiinflammatory; asthma

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