engleski

Macrolactonolides: a novel class of anti- inflammatory compounds

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.

concept; anti-inflammatory; glucocorticoid; macrolides

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