Synthesis and analgesic activity of N,N '-dicarbonyltryptamines

Citation
Dm. Han et al., Synthesis and analgesic activity of N,N '-dicarbonyltryptamines, PREP BIOC B, 30(3), 2000, pp. 231-240
Citations number
6
Categorie Soggetti
Biochemistry & Biophysics
Journal title
PREPARATIVE BIOCHEMISTRY & BIOTECHNOLOGY
ISSN journal
10826068 → ACNP
Volume
30
Issue
3
Year of publication
2000
Pages
231 - 240
Database
ISI
SICI code
1082-6068(2000)30:3<231:SAAAON>2.0.ZU;2-B
Abstract
5-Methoxytryptamine and L-tryptophan methyl ester were acylated with maloni c acid, dimethyl malonate, or succinic anhydride to produce the correspondi ng N, N'-dicarbonyl-tryptamine derivatives. The analgesic activity was eval uated by the tail flick test. All of the compounds exhibited desirable anal gesic potency. This result is consistent with that of N-(N-acetyl-L-tryptop hanyl)-5-methoxytryptamine and confirmed that introducing substituted trypt amine into the amide chain of melatonin does enhance analgesic potency.