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Patent Summary
Halogenated PGE derivatives which display enhanced stability relative to those previously disclosed [101] are claimed. They possess good cytoprotective and antisecretory effects, whilst displaying fewer side-effects characteristic of prostaglandins.
The cytoprotective activity was determined against ethanol-induced ulcerations in rats whilst inhibition of gastric acid secretion was demonstrated in a gastric pouch model in beagles, over a 4 hour period. Most of the compounds did not induce diarrhoea in rats at 3.2mg/kg (ig). The preferred example had a minimum effectual dose of 1 μg/kg (po) in rats and an ED50 of 0.03 μg/kg (ig) in dogs. Data are provided for all examples.
The disclosure is illustrated by ten compounds which are prepared via conventional Wittley and organocuprate reactions. A variety of methods are employed for producing the desired degree of fluorination. Methyl 7-[2β-[6-(1-cyclopenten-1-yl)-4R-(fluoromethyl)-4-hydroxy-1E,5E-hexadienyl]-3α-5-oxo-1R, 1α-cyclopentyl] -4Z-heptenoate is the only specifically claimed compound.