Abstract
Amino acids are safe molecules with variable efficacy against ulceration. Considering the good antioxidant potential of N-aroyl- N, N'-dicyclohexyl urea and antiulcer activities of amino acids, a series of amino acid conjugates of N-aroyl- N, N'-dicyclohexyl urea was synthesized and the effect against ulceration in albino rats induced by pyloric ligation was screened. All these compounds were found to be safe and active. Reduction of ulcer index was significant for all compounds. Conjugates of methionine and histidine exhibited enhanced antiulcer activity comparable to omeprazole in terms of inhibition of release of gastric juice, hydrochloric acid and neutralization activity. The promising efficacy and safety of these compounds is interesting for further investigation.
Highlights
Intraduodenal administration of mixed amino acid solution has been reported to significantly inhibit gastric acid secretion and gastrin release, stimulated by intragastric perfusion of peptone [1]
Equimolar quantity of benzoic acid and DCC were used with triethylamine (TEA) as catalyst
Reaction of dry toluene in presence of TEA generated the carboxylate anion that acted as nucleophile to undergo nucleophillic addition with DCC to give the O-aryl intermediate that upon rearrangement yielded the urea analogue N-cyclohexyl-N-(cyclohexylcarbamoyl) benzamide
Summary
Intraduodenal administration of mixed amino acid solution has been reported to significantly inhibit gastric acid secretion and gastrin release, stimulated by intragastric perfusion of peptone [1]. The reaction between amino acids and halohydrocarbon has been reported being carried out in presence of K2CO3 using methanol as solvent [15].
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