Synthesis and anti-ulcer activities of sodium alkylazulene sulfonates.
- 1 January 1988
- journal article
- research article
- Published by Pharmaceutical Society of Japan in CHEMICAL & PHARMACEUTICAL BULLETIN
- Vol. 36 (2) , 641-647
- https://doi.org/10.1248/cpb.36.641
Abstract
Many derivatives of sodium alkylazulene sulfonates were newly synthesized and their antiulcer activities were examined in Shay pylorus-ligated rats. The values of lipophilicity (log P), a physicochemical parameter, of these new azulene derivatives were also examined in order to study the structure-activity relationship. The optimum value of log P which gave maximum anti-ulcer activity was about -1.0. Among the derivatives of azulene examined, 3-ethyl-7-isopropylazulene-1-sulfonic acid sodium salt (KT1-32) exhibited an extremely potent inhibitory action against Shay ulcer, and its antipeptic activity was more potent than that of guaiazulene sodium sulfonate (GAS). Furthermore, KT1-32 was extremely stable on heating as compared to GAS.This publication has 1 reference indexed in Scilit:
- PROTEIN MEASUREMENT WITH THE FOLIN PHENOL REAGENTJournal of Biological Chemistry, 1951