2. Academic Validation
  3. Macrolactonolides: a novel class of anti-inflammatory compounds

Macrolactonolides: a novel class of anti-inflammatory compounds

  • Bioorg Med Chem. 2013 Jan 1;21(1):321-32. doi: 10.1016/j.bmc.2012.10.036.
Linda Tomašković 1,  Marijana Komac,  Oresta Makaruha Stegić,  Vesna Munić,  Jovica Ralić,  Barbara Stanić,  Mihailo Banjanac,  Stribor Marković,  Boška Hrvačić,  Hana Čipčić Paljetak,  Jasna Padovan,  Ines Glojnarić,  Vesna Eraković Haber,  Milan Mesić,  Mladen Merćep
Affiliations

Affiliation

  • 1 GlaxoSmithKline Research Centre Limited, Prilaz baruna Filipovića 29, HR-10000 Zagreb, Croatia. Linda.Tomaskovic@glpg.com
PMID: 23199485 DOI: 10.1016/j.bmc.2012.10.036
Abstract

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.

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