Synthesis and pharmacological evaluation of (indol-3-yl) alkylamides as potent analgesic agents

Authors
Fouchard, F Marchand, P Le Baut, G Emig, P Nickel, B
Citation
F. Fouchard et al., Synthesis and pharmacological evaluation of (indol-3-yl) alkylamides as potent analgesic agents, ARZNEI-FOR, 51(10), 2001, pp. 814-824
Citations number
15
Categorie Soggetti
Pharmacology & Toxicology
Journal title
ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH
ISSN journal
00044172 → ACNP
Volume
51
Issue
10
Year of publication
2001
Pages
814 - 824
Database
ISI
SICI code
0004-4172(2001)51:10<814:SAPEO(>2.0.ZU;2-A
Abstract
A series of (indol-3-yl)alkylamides was synthesized and evaluated for analg esic activity. Two N-(pyridin-4-yl)acetamides, compounds 24 and 25, bearing benzyl or 4-fluorobenzyl moieties in I-position of indole ring exhibited p romising analgesic properties (ED50 = 8.1 and I I mg/kg p.o., respectively) , being as potent as the reference drugs flupirtine (CAS 56995-20-1), ibupr ofen (CAS 15687-27-1) and diclofenac (CAS 15307-86-5). The two test compoun ds were tested for their anti-inflammatory activity by carrageenin-induced edema In rat paw test. 4-Fluorobenzyl derivative 25 whose ID50 was 0.085 +/ - 0.021 mmol/kg was selected as a lead compound for further pharmaco-modula tion.