SYNTHESIS, GASTROPROTECTIVE, ANTISECRETORY AND ANTI-HELICOBACTER EFFECT OF PIPERIDINYLMETHYL)PHENOXY)PROPYL]-HYDROXYACETAMIDE 2-HYDROXYPROPANE-1,2,3-TRICARBOXYLATE BISMUTH(3(-MX(1)()) COMPLEX (MX(1)))

MX(1) piperidinylmethyl)phenoxy)propyl]-hydroxyacetamide 2-hydroxyprop ane-1,2,3-tricarboxylate bismuth (3(+)) complex) is a novel salt of th e active metabolite of H-2-antagonist roxatidine with a complex of bis muth with citric acid. In a model of ethanol-induced ulcers in male Wi star rats, both roxatidine and the bismuth salt reduced the number and the total length of lesions. Comparison of roxatidine and MX(1) at eq uimolar doses of 160 mu mol kg(-1) showed a more potent cytoprotective effect of MX(1). The potency of anti-secretory and antiacidic effects of MX(1) was more than twice that of roxatidine on histamine-stimulat ed secretion in female Wistar pylorus-ligated rats. Microbiological te sts with the reference bismuth preparation De-Nol showed prominent ant i-Helicobacter properties of MX(1) in-vitro. Both test compounds had s imilar range of MICs to Helicobacter pylori, from 4 to 64 mu g bismuth mL(-1). The cytoprotective, antisecretory, anti-acidic and anti-Helic obacter properties of the new agent MX(1) warrant further more extensi ve pharmacological and clinical trials.