N-Pyridinyl(methyl)-indole-1- or 3-propanamides and propenamides acting as topical and systemic inflammation inhibitors.
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.
Dassonville
Alexandra
A
Pharmacochemistry Department, Faculty of Pharmacy, Nantes University, Nantes Atlantique Universities, IICiMed UPRES EA 1155, Nantes, France.
Lardic
Morgane
M
Breteche
Anne
A
Nourrisson
Marie Renee
MR
Le Baut
Guillaume
G
Grimaud
Nicole
N
Petit
Jean-Yves
JY
Duflos
Muriel
M
D000577:Amides / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D003907:Dexamethasone; D007052:Ibuprofen; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D007249:Inflammation / Q000188:drug therapy* / Q000517:prevention & control; D051379:Mice; D013329:Structure-Activity Relationship
D000577:Amides; D007211:Indoles; D003907:Dexamethasone; D007052:Ibuprofen