[Synthesis of 2-hydroxyl-5-butyramidobenzoic acid and its effect on acetic acid-induced colitis in rats].
OBJECTIVE
To study the method for synthesis of 2-hydroxyl-5- butyramidobenzoic acid and test its effect on acetic acid-induced colitis in rats.


METHODS
2-hydroxyl-5-butyramidobenzoic acid was synthesized from 5-aminosalicylic acid and butyric acid by amidation, esterification and hydrolization. The effect of 2-hydroxyl-5-butyramidobenzoic acid on acetic acid enema-induced colitis in rats was investigated.


RESULTS
The structure of 2-hydroxyl-5-butyramidobenzoic acid was identified by IR and 1H-NMR. After treatment with acetic acid, the colon mucosal damage index (CMDI), fecal occult blood (OB) test, and activity of myelperoxidase (MPO) increased significantly in the rats as compared to the control levels. 2-hydroxyl-5- butyramidobenzoic acid obviously reduced the CMDI and OB, and reduced the level of MPO in the rats with colitis.


CONCLUSIONS
The synthesis of 2-hydroxyl-5-butyramidobenzoic acid requires only mild conditions with simple procedures, and the synthesized 2-hydroxyl-5-butyramidobenzoic acid shows obvious therapeutic effects on mucosal damage of in rats with acetic acid-induced colitis.
Department of Pharmacy, Xi'an Jiaotong University College of Medicine, Xi'an, China. skcy@stu.xjtu.edu.cn
Rui-cai
RC
Shi
Jian-feng
JF
Xing
Zhao-guo
ZG
Liu
Zhi-zhao
ZZ
Yuan
San-qi
SQ
Zhang
Xiao-li
XL
Bian
Ai-guo
AG
Zeng
D019342:Acetic Acid; D062365:Aminobenzoates / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D003093:Colitis, Ulcerative / Q000139:chemically induced / Q000188:drug therapy*; D008297:Male; D020011:Protective Agents / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D051381:Rats; D017207:Rats, Sprague-Dawley; D012459:Salicylates
C557054:5-(butanoylamino)-2-hydroxy-benzoic acid; D062365:Aminobenzoates; D020011:Protective Agents; D012459:Salicylates; D019342:Acetic Acid