219544-69-1Relevant articles and documents
Synthesis and pharmacological evaluation of (indol-3-yl)alkylamides as potent analgesic agents
Fouchard,Marchand,Le Baut,Emig,Nickel
, p. 814 - 824 (2007/10/03)
A series of (indol-3-yl)alkylamides was synthesized and evaluated for analgesic activity. Two N-(pyridin-4-yl)acetamides, compounds 24 and 25, bearing benzyl or 4-fluorobenzyl moieties in 1-position of indole ring exhibited promising analgesic properties (ED50 = 8.1 and 11 mg/kg p.o., respectively), being as potent as the reference drugs flupirtine (CAS 56995-20-1), ibuprofen (CAS 15687-27-1) and diclofenac (CAS 15307-86-5). The two test compounds 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 pharmacomodulation.
(1-Benzylindole-3-yl)alkanoic acids; novel nonsteroidal inhibitors of steroid 5α-reductase (I)
Sawada, Kozo,Hirai, Hideo,Golden, Patrick,Okada, Satoshi,Sawada, Yuki,Hashimoto, Masashi,Tanaka, Hirokazu
, p. 1683 - 1687 (2007/10/03)
A novel series of indole-3-alkanoic acids with varied N-benzyl substituents were synthesized as nonsteroidal inhibitors of steroid 5α- reductase. The structure-activity relationships in this series were studied and the optimum carboxylic acid side chain w
