Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 11, Pages 3373-3376Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.04.004
Keywords
(8R,9S)-8,9-Dihydro-6,9-epoxy-8,9-anhydropseudoerythromycin A (EM900); Anti-inflammatory agent; Immunomodulatory agent; 14-Membered non-antibiotic macrolide; Diffuse panbronchiolitis
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Funding
- Grants-in-Aid for Scientific Research [21590046, 22890175, 21590122, 22790017] Funding Source: KAKEN
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Herein, we report the design and synthesis of the novel 12-membered non-antibiotic macrolide (8R,9S)-8,9- dihydro-6,9-epoxy-8,9-anhydropseudoerythromycin A (EM900), which was found to be a potent anti-inflammatory and/or immunomodulatory agent, capable of promoting monocyte to macrophage differentiation. This molecule shows improved acid stability, does not exhibit any anti-bacterial activity and has relatively low cytotoxicity against THP-1 cells. In addition, one of its analogues, (8R, 9S)-4 '',13-O-diacetyl- 8,9-dihydro-6,9-epoxy-8,9-anhydropseudoerythromycin A (EM911), was found to be twice as effective as EM900. (C) 2011 Elsevier Ltd. All rights reserved.
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