Publications by authors named "Anne Breteche"
A short, convergent, and selective synthesis of meiogynin A, an inhibitor of the antiapoptotic protein Bcl-xL, has been performed. This synthesis, based on a biomimetic approach, allowed the determination of its absolute configuration. Three isomers of meiogynin A have also been elaborated.
View Article and Find Full Text PDFThe phospholipid fatty acid composition of the North-East Atlantic sponge Polymastia penicillus (South Brittany, France) was investigated. Sixty fatty acids (FA) were identified as methyl esters (FAME) and N-acyl pyrrolidides (NAP) by gas chromatography-mass spectrometry (GC/MS), including eight Delta5,9 unsaturated FA and three long-chain 2-hydroxylated FA. The major phospholipid FA were palmitic (14.
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- The study presents a method for creating new non-acidic NSAIDs from N-pyridinyl(methyl)indolylpropanamides.
- Pharmacomodulation was applied at specific sites on the indole ring and propanamide chain to enhance effectiveness.
- One of the synthesized compounds, N(3)-pyridinylmethyl-[1(4-chlorobenzyl-5-chloroindol-3-yl)propanamide], showed greater activity than ibuprofen and similar potency to dexamethasone in a mouse ear swelling test.
The authors have described the synthetic way to new N-pyridinyl(methyl)indolylpropanamides acting as non acidic NSAIDs. Pharmacomodulation was carried out at N-1 and C-5 of the indole ring and at the level of the propanamide chain. N-(pyridin-3-ylmethyl)-3-[5-chloro-1-(4-chlorobenzyl)-indol-3-yl]propanamide 32 represents one of the most potent compounds evaluated in the TPA-induced mouse ear swelling assay, with a level of activity higher than that of ibuprofen and comparable to that of dexamethasone.
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- A series of N-substituted indole carboxamides were synthesized to evaluate their effectiveness as inflammation inhibitors, with only two compounds showing significant effects in reducing inflammation.
- The study revealed that incorporating alkyl chain spacers improved the efficacy of these compounds, particularly in the indolepropanamide sub-group.
- The most effective propanamides demonstrated potent anti-inflammatory properties in both oral and topical applications, with one compound showing up to 78% inhibition in a mouse ear swelling assay.