Anti-ulcer agents

The Camps reaction has been used to prepare a variety of anti-ulcer agents of the type 23. As can be seen from the yields, the reaction works equally well with electron donating and withdrawing aromatic rings. ... 

Progressive departure from the fundamental structure of the lead agent cimetidine led to the anti ulcer agent oxmetidine (47). The synthesis involves -methylation (CH3I) of the 2-thiouracil intermediate and is followed by an addition-elimination reaction with 2-(5-methyl-4-imidazolylmethylthio) ethylamine to give oxmetidine (47). ... 

An aryloxypyrimi done has been described as an anti ulcer agent this activity is of note since the agent does not bear any structural relation to better known anti ulcer drugs. Displacement of halogen on the acetal of chloro-acetaldehyde by alkoxide from m-cresol gives the intermediate This affords enaminoaldehyde when subjected... 

Yoshikawa, T., Naito, Y., Tanigawa, T. and Kondo, M. (1993). Free radical scavei ng activity of the novel anti-ulcer agent rebamipide studied by electron spin resonance. Arzneim-Forsch. 43, 363-366. 

Azolides used as inhibitors for monoamine oxidase1171 or human leucocyte elastase,1181 as inductors of recessive lethal genes in Drosophila,1191 as histamine H2-receptor antagonists,1201 as anti-ulcer agents,1211 or as pharmacophores for anthelmintic, analgesic, and antimicrobial activity 1221... 

The anti-ulcer agents omeprazole, lanzoprazole, and pantoprazole have been introduced during the past decade for the treatment of peptic ulcers. Gastric acid secretion is efficiently reduced by prazole inhibition of H+K+-ATPase in the parietal cells of the gastrointestinal mucosa [75]. The prazoles themselves are not active inhibitors of the enzyme, but are transformed to cyclic sulfenamides in the intracellular acidic compartment of parietal cells [76]. The active inhibitors are permanent cations at pH < 4, with limited possibilities of leaving the parietal cells, and thus are retained and activated at the site of action. In the neutral body compartments the prazoles are stable, and only trace amounts are converted to the active drugs. (For a review on omeprazole, see Ref. [77].)... 

Misoprostol C22H38Os 382.5 immunosuppressive agent Anti-ulcer agent... 

Due to the large number of references which appeared to be worth mentioning, it became necessary to divide this review into two parts. The present part deals mainly with pyridazines as chemotherapeutics, antithrombotics, antise-cretory and anti-ulcer agents, analgesic and anti-inflammatory agents as well as with various central nervous system stimulants and depressants. Part 2 of this review, which is planned for a future volume of this Series, will be devoted mainly to compounds which act on the cardiovascular system and to a discussion of miscellaneous additional pharmacological activities of pyridazine derivatives. 

The most potent among the compounds tested were the pyridazi-nones (28, R1 = Ph, R2, R3, R4, R5 = H, n = 2-5) [101]. Structure-activity relationships have been investigated in detail with this type of compound. Also, thio-analogues of compounds (28) (3-pyridazinethione derivatives) as well as 2-aminoalky]-6-aryl-3(2//)-pyridazinones were claimed in patents as gastric secretion inhibitors or anti-ulcer agents [100, 102, 103]. 

The procedure has been used for the synthesis of potential anti-ulcer agents [Scheme 5.19, R = (CH2) NH2)] via the phthalimido derivative, and R = (CH2) CSNR2 via the cyano derivatives [73,74],... 

Cyanoethyl derivatives of 1-alkyl and 1,3-dialkyl-6-amino uracils (LXX) are reported to have activity as anti-ulcer agents. Inhibition of appetite and hypo-cholesterolemic activity are also claimed [437]. 

Specify the configuration of the stereogenic units in the anti-ulcer agent trimoprostil. 

Anti-ulcer agent Gastrointestinal agent Serotonin agonist... 

Anti-infective agent Anti-ulcer agent Enzyme inhibitor... 

Deoxy-16-phenoxy-17,18,19,20-tetranor-PGEj (111a) is a potent and selective anti-ulcer agent. It has been prepared from... 

In addition to this marked reduction in toxicity, some of these complexes were found to be potent anti-ulcer agents. Since it is well-known that clinically used anti-arthritic drugs cause ulcers and gastrointestinal distress, the observed anti-ulcer activity further distinguishes these coordination compounds from their parent compounds as being safer and potentially much more therapeutically useful than the currently used drugs. 

Copper complexes are a unique class of anti-arthritic drugs for 2 important reasons. First, animal studies have revealed that they are potent anti-ulcer agents... 

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