A series of 9 phenoxyacetic acids substituted in the o-, m-, and p-position of benzene ring with 2-(2-oxo-1-azacycloalkyl)acetamidic moiety containing 5-7-membered -lactam ring was prepared by a 4-step synthetic procedure. Five selected substances of this series were tested in vitro for inhibition of porcine kidney aminopeptidase M. 2-{4-[2-(2-Oxoperhydroazepin-1-yl)acetamido]phenoxy}acetic acid exhibited the highest activity with K i = 243.6 M.
A wide range of dyspeptic symptoms in clinical practice reflect the high prevalence of functional disorders of the gastrointestinal (GI) tract. Prokinetic agents are the current mainstay in the therapy of functional dyspepsia. One of these drugs is itopride. We evaluated therapeutic efficacy of itopride according to the literature review. The therapeutic potential of itopride is connected with a dual effect: influencing of enzyme acetylcholinesterase activity and blocking dopamine D2 receptors. After the itopride administration, the contractility of smooth muscle in the upper GI tract increases. Itopride is a drug with rapid absorption from the small bowel; its peak serum concentration occurs 35 minutes after oral administration. Itopride does not pass the blood-brain barrier and does not affect the heart rate by influencing the QT segment. Itopride is a safe prokinetic agent with positive influence on the symptoms of functional dyspepsia such as postprandial fullness, bloating, and gastric emptying. Itopride could also be used for the therapy of the mild form of gastro-oesophageal reflux.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.