Synthesis of pro-drug of salicylic acid saccharide carboxylate and evaluation of their analgesic activity
WU Xue-fen
FANG Xiao-yan
LI Wei
HOU Yi-min
SUN De-mei
Abstract：Objective: To prepare salicylic acid saccharide carboxylate and evaluate their irritation activity and analgesic activity. Methods: The salicylic acid saccharide carboxylate were prepared through carboxylic acid-or-ganic alkali and carboxylic salts, and the acetylated salicylic glucopyranose tetraacetate was synthesized by sequen-tial elution. The structures of the products were identified by ~1H-NMR and IR. The anticoagulant activity and analge-sic activity were respectively evaluated by cutting tail in mice and the mice twist test, and the irritation activity was observed by tissue slices. Results: Fine β-onfiguration salicylic acid saccharide carboxylate were prepared and anti-coagulant activity and analgesic activity were obtained. The irritation of the prepared products was less than the pri-mary drug and aspirin. Conclusion: The methods of arboxylic salts and sequential elution were firstly applied to the preparation of salicylic acid saccharide carboxylate and acetylated salicylic glucopyranose tetraacetate. The methods were operated easily and superior to the phase-transfer catalysis method. The preparation of salicylic acid saccharide carboxylate could increase the anticoagulant activity and analgesic activity and reduce the irritation of their corre-sponding primary drug.
Keywords：salicylic acidsaccharide carboxylateanticoagulant activityanalgesicirritation
Publication Date：2009-01-01
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：7( 2353-2359 )