N-Pyridinyl(methyl)-indole-1- or 3-propanamides and propenamides acting as topical and systemic inflammation inhibitors
Autor: | J. Y. Petit, Morgane Lardic, Guillaume Le Baut, Anne Breteche, Muriel Duflos, Marie Renee Nourrisson, Alexandra Dassonville, N. Grimaud |
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Rok vydání: | 2008 |
Předmět: |
Inflammation
Pharmacology Indole test Indoles Ear swelling Stereochemistry Ibuprofen General Medicine Systemic inflammation Amides Propanamide Dexamethasone Mice Structure-Activity Relationship chemistry.chemical_compound chemistry Drug Discovery medicine Animals Structure–activity relationship medicine.symptom medicine.drug |
Zdroj: | Journal of Enzyme Inhibition and Medicinal Chemistry. 23:728-738 |
ISSN: | 1475-6374 1475-6366 |
DOI: | 10.1080/14756360802208251 |
Popis: | 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 N(1) and C(5) of the indole ring and at the level of the propanamide chain. N(3)-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. |
Databáze: | OpenAIRE |
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