Macrolactonolides: a novel class of anti-inflammatory compounds

Bioorganic & Medicinal Chemistry
Linda TomaškovićMladen Merćep

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.

References

Dec 1, 1991·Antimicrobial Agents and Chemotherapy·L E BermudezL S Young
Jan 14, 2004·The Journal of Pharmacology and Experimental Therapeutics·Michael StoeckDaniela S Bundschuh

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Citations

Mar 19, 2014·Pharmacology & Therapeutics·Michael J ParnhamRobin Vos
Jun 5, 2014·Future Medicinal Chemistry·Vesna Eraković HaberGoran Kragol
Oct 2, 2015·Beilstein Journal of Organic Chemistry·Ana ČikošSulejman Alihodžić
Sep 30, 2016·Inflammation Research : Official Journal of the European Histamine Research Society ... [et Al.]·Michael J Parnham
Aug 3, 2019·The Veterinary Record·Sophie Mainguy-SeersJean-Pierre Lavoie
Oct 31, 2021·Pharmacological Reviews·Jennifer A KrickerMichael J Parnham

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