期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 4, 页码 1382-1387出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.01.013
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资金
- NHLBI NIH HHS [R01 HL079312, R01-HL079312] Funding Source: Medline
- NIDCR NIH HHS [P50 DE016191, P50-DE-016191] Funding Source: Medline
A new class of chemically and metabolically stable lipoxin analogs featuring a replacement of the tetraene unit of native LXA(4) with a substituted benzo-fused ring system have been designed and studied. These molecules were readily synthesized via a convergent synthetic route involving iterative palladium-mediated cross-coupling, and exhibit enhanced chemical stability, as well as resistance to metabolic inactivation via eicosanoid oxido-reductase. These new LX analogs were evaluated in a model of acute inflammation and were shown to exhibit potent anti-inflammatory properties, significantly decreasing neutrophil infiltration in vivo. The most potent among these was compound 9 (o-[9,12]-benzo-15-epi-LXA(4) methyl ester. Taken together, these findings help identify a new class of stable and easily prepared LX analogs that may serve as novel tools and as promising leads for new anti-inflammatory agents with improved therapeutic pro. le. (c) 2008 Elsevier Ltd. All rights reserved.
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