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N-Pyridinyl(methyl)-indole-1- or 3-propanamides and propenamides acting as topical and systemic inflammation inhibitors |
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| Authors: | Alexandra Dassonville Morgane Lardic Anne Breteche Marie Renee Nourrisson Guillaume Le Baut Nicole Grimaud |
| Institution: | 1. Pharmacochemistry Department, Faculty of Pharmacy, Nantes University, Nantes Atlantique Universities, IICiMed UPRES EA 11551 rue Gaston VeilF-44035, Nantes, France;2. Immuno-Pharmacology Department, Faculty of Pharmacy, Nantes University, Nantes Atlantique Universities, IICiMed UPRES EA 11551 rue Gaston Veil, F-44035, Nantes, France |
| Abstract: | In this study, the synthetic way to new N-pyridinyl(methyl)indolylpropanamides acting as non acidic NSAIDs has been described. Pharmacomodulation was carried out at N1 and C5 of the indole ring and at the level of the propanamide chain. N3-pyridinylmethyl-1(4-chlorobenzyl-5-chloroindol-3-yl)propanamide represents one of the most potent compounds in the TPA-induced mouse ear swelling assay, with a level of activity higher than that of ibuprofen and comparable to that of dexamethasone. |
| Keywords: | N-pyridinyl and N-pyridinylmethyl-indole-1-or-3-propanamides and propenamides topical and systemic inflammation inhibitors |