Gastric acid secretion inhibitors

Use peptic ulcer therapeutic, gastric acid secretion inhibitor... 

Mecftanism of Action AGI Hj-blocker and gastric acid secretion inhibitor that inhibits histamine action at histamine 2 receptors of parietal cells Therapeutic Effect Inhibits gastric acid secretion when fasting, at night, or when stimulated by food, caffeine, or insulin. 

P. Lindberg, P. Norberg, T. Ahninger, A. Brandstram, B. Wallmark (1986). The mechanism of action of the gastric acid secretion inhibitor omeprazole. J. Med. Chem. 29 1327-1329. 

The development of the single enantiomer azole within the family of compounds used for gastrointestinal treatments is exemplified by Astra-Zeneca s Esomeprazole (a potent gastric acid secretion inhibitor) (Eigure 1.54). This development gave the impetus for the search for industrial chiral sulfoxidation catalysts. 

The structures of all currently approved gastric acid secretion inhibitors that act as inhibitors of the sodium-potassium pump consists of variously substituted pyiidylsulfonyl-benzimidazoles. A structurally very distinct compound based on a pyrimidine moiety has much the same activity as the benzimidazole-based drugs. In yet another convergent synthesis, reaction of (3-phenethylamine (53) with acetic anhydride affords amide 54. Treatment with polyphosphoric acid (PPA) then leads to ring closure to form the dihydroisoquinoline (55). Sodium borohydride then reduces the enamine function to afford fragment 56. 

Proton pump inhibitors (gastric acid secretion inhibitors, gastric add pump inhibitors) inhibit gastric acid secretion 90% greater than the H2 blockers because they block the final step of acid production. Both omeprazole (Prilosec) and lansoprazole (Prevacid) are proton pump inhibitors used for the treatment of peptic ulcers and GERD. Those with hepatic impairment should take these drags with caution and have liver enzymes monitored regularly. 

Omeprazole and its (5)-isomer, esomeprazole 144 (Fig. 12.8) belongs to a class of potent gastric acid secretion inhibitors and are used as antiulcer agents. The skeleton... 

An application of the Kagan-Modena procedure for the synthesis of the enantio-merically pure S enantiomer of omeprazol was reported by Cotton et ol. [69] This enantiomer is called esomeprazol and is the active component of Nexium . It is a highly potent gastric acid secretion inhibitor. 

Bemtsson P, Brandstrom A, Palmer L, Sjostrand SE, Sundell G (1977) Gastric acid secretion inhibitors II. Carbamates and aromatic alcohols and phenols. Acta Pharm Suecia 14 229-236... 

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