Syntheses and antiinflammatory activity of malonamic acid, malonamate and malonamide derivatives of some heterocyclic compounds.
- 1 January 1985
- journal article
- research article
- Published by Pharmaceutical Society of Japan in CHEMICAL & PHARMACEUTICAL BULLETIN
- Vol. 33 (11) , 4878-4888
- https://doi.org/10.1248/cpb.33.4878
Abstract
Malonamate, malonic acid and malonamide derivatives of heterocyclic compounds were synthesized as part of a search for new biologically active compounds, e.g., those having antiinflammatory activity. Malonamates (1-17) were prepared by the reaction of amines containing heterocycles with malonic acid monoethyl ester. Hydrolysis of the malonamates gave the malonamic acids (18-24) in good yields. Malonamides (25-43) were synthesized by condensing amines with N-substituted malonamic acids. The antiinflammatory activity of these compounds was examined against carrageenin-induced rat paw edema. N-[2-(6-Methoxyl)benzothiazolyl]malonamic acid (23) and its ethyl ester (7) showed significant activity.This publication has 1 reference indexed in Scilit:
- Carrageenin-Induced Edema in Hind Paw of the Rat as an Assay for Antiinflammatory DrugsExperimental Biology and Medicine, 1962