Publications by authors named "Nicole Grimaud"
Article Synopsis
- 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.
Three marine alkaloids, purified from Clavelina moluccensis, were structurally identified as lepadiformines A, B, and C and studied on frog atrial myocytes I(K1), using the patch-clamp technique. Lepadiformine A (0.4 to 3.
View Article and Find Full Text PDFThe 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.
View Article and Find Full Text PDFN-Pyridinyl(methyl)-N1-substituted-3-indolepropanamides (17-32) were prepared starting from the corresponding acids and screened for their anti-inflammatory activity. Pharmacomodulation was carried out on the indole and amidic nitrogens by incorporation of substituents associated with higher potency in previously synthesized related 3-indolepropanamides series. In the inhibition of topical inflammation determined by reduction of ear thickness in the acute PMA mouse ear swelling test, high levels of activity (ID50 approximately 0.
View Article and Find Full Text PDFArticle Synopsis
- 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.