Studies on fused indoles. II. Structural modifications and analgesic activity of 4-aminomethyltetrahydrothiopyrano(2,3-b)indoles.
- 1 January 1984
- journal article
- research article
- Published by Pharmaceutical Society of Japan in CHEMICAL & PHARMACEUTICAL BULLETIN
- Vol. 32 (3) , 877-886
- https://doi.org/10.1248/cpb.32.877
Abstract
A series of 4-aminomethyl-2, 3, 4, 9-tetrahydrothiopyrano [2, 3-b] indole derivatives was synthesized and evaluated for analgesic activity. Preliminary structure-activity relationship analysis showed that substitution on the benzene portion of the indole ring reduced the analgesic activity, whereas a short-chain Nb-alkyl substituent enhanced the potency, as exemplified by an Nb-methyl substituted analogue. This compound was equipotent to morphine in the acetic acid writhing assay using mice.Keywords
This publication has 2 references indexed in Scilit:
- A Method for Evaluating both Non-Narcotic and Narcotic AnalgesicsExperimental Biology and Medicine, 1957
- A METHOD FOR MEASUREMENT OF ANALGESIC ACTIVITY ON INFLAMED TISSUE1957