Anti-ulcerants

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). ... 

Another entry into the anti ulcer sweepstakes is etinfidine (50). It is synthesized by displacement of halide from 4-chloromethyl-5-methylimidazole (4 ) with substituted thiol The latter is itself made from thiourea analogue by an addition-elimination reaction with cysteamine 52. °... 

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... 

Figure 6 from Carbohydrate Research, vol 311, Sakurai MH, Kiyohara H, Matsumoto T, TsumurayaY, Hashimoto Y, Yamada H (1998) Characterization of antigenic epitopes in anti-ulcer pectic polysaccharides from Bupleurum falcatum L. using several carbohy-drases. p 219-p229, all with permission from Elsevier... 

S)-a-substituted P-bromo-a-hydroxy acids (S)-4 are very important chiral synthon for medicinally important compounds, such as potential new hypoglycemia active alkylglycidic acids (ref. 1) and anti-ulcer active misoprost (ref. 2). 

Stimulation of macrophage phagoc3dosis Anti-ulcer activity... 

The search for specific inhibitors of gastric H,K-ATPase has a dual purpose. First, with the help of suitable inhibitors it is possible to get insight into the molecular mechanisms of H,K-ATPase, and second, a specific inhibitor might be clinically useful for inhibition of gastric acid secretion in anti-ulcer therapy. 

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. 

Antitussive drugs, 3 (1963) 89 Anti-ulcer drugs, of plant origin, 28 (1991) 201... 

Approximately, 2 5 million Americans are affected by PUD, with the lifetime prevalence estimated to be 12% in men and 10% in women.2 Annual direct and indirect costs associated with PUD in the United States are estimated to be more than 9 billion. Despite the widespread use of conventional anti-ulcer therapy that effectively reduces gastric acid secretion, ulcers frequently recur, with 1-year recurrence rates (after ulcer initial healing) estimated to range from 60% to 100%.1... 

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].)... 

A closely related coupling reaction is a key step in a synthesis of the anti-ulcer prostaglandin 1, a synthesis that was developed for large scale preparation of this compound.1 2 3 4 5... 

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 most potent activities (gastric antisecretory activity in the pylorus-ligated rat or anti-ulcer activity on stress-induced gastric lesion in rat) have been observed with compounds (30), (31) [106], (32) [107], (33) and (34) [108], which were shown neither to be histamine H2 receptor inhibitors nor to act as anticholinergic agents. Thus, the activity of compound (32), for example, has been reported to be superior to that of cimetidine [107],... 

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],... 

Shibata, H., Nagaoka, M., Takeuchi, Y., Hashimoto, S., Ueyama, S., and Yokokura, T. (1998). Anti-ulcer effect of fucoidan from brown seaweed, Cladosiphon okamuranus Tokida. ]pn. Pharmacol. Ther. 26,1211-1215. 

Misoprostol (Cytotec) Anti-ulcer Tab 100, 200 mg 100-200 mg qid reduce dosage if diarrhea abortifacient, contraception mandatory. 

Digestive system (7.3) Antiacids/anti-ulcerous 4 Omeprazol 7... 

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