Synthesis and gastroprotective activity of 4H-pyrido[1,2-a]pyrimidin-4-ones. 1992

I Hermecz, and J Sipos, and L Vasvári-Debreczy, and K Gyires, and Z Kapui
Chinoin Pharmaceutical and Chemical Works Ltd., Budapest, Hungary.

The cytoprotective effect of different types of 4h-pyrido[1,2-a]pyrimidin-4-one derivatives was investigated. Short synthesis of the investigated compounds was depicted. The gastroprotective effect was determined against acidified ethanol induced mucosal lesions in rats. The most effective compounds belong to unsaturated 4-oxo-4h-pyrido[1,2-a]pyrimidine-3-carboxamide derivatives, and the most active one contains a methyl group in position 6 and a cyclopentyl group on the nitrogen of the carboxamide group. Further pharmacological, biochemical and clinical studies may justify, that the representative of this type of compounds may be useful as prophylactic agents against gastric damage caused by non-steroidal antiinflammatory agents.

UI MeSH Term Description Entries
D007213 Indomethacin A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES. Amuno,Indocid,Indocin,Indomet 140,Indometacin,Indomethacin Hydrochloride,Metindol,Osmosin
D011744 Pyrimidinones Heterocyclic compounds known as 2-pyrimidones (or 2-hydroxypyrimidines) and 4-pyrimidones (or 4-hydroxypyrimidines) with the general formula C4H4N2O. Pyrimidinone,Pyrimidone,Pyrimidones
D002927 Cimetidine A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output. Altramet,Biomet,Biomet400,Cimetidine HCl,Cimetidine Hydrochloride,Eureceptor,Histodil,N-Cyano-N'-methyl-N''-(2-(((5-methyl-1H-imidazol-4-yl)methyl)thio)ethyl)guanidine,SK&F-92334,SKF-92334,Tagamet,HCl, Cimetidine,Hydrochloride, Cimetidine,SK&F 92334,SK&F92334,SKF 92334,SKF92334
D003663 Decision Trees A graphic device used in decision analysis, series of decision options are represented as branches (hierarchical). Decision Tree,Tree, Decision,Trees, Decision
D000431 Ethanol A clear, colorless liquid rapidly absorbed from the gastrointestinal tract and distributed throughout the body. It has bactericidal activity and is used often as a topical disinfectant. It is widely used as a solvent and preservative in pharmaceutical preparations as well as serving as the primary ingredient in ALCOHOLIC BEVERAGES. Alcohol, Ethyl,Absolute Alcohol,Grain Alcohol,Alcohol, Absolute,Alcohol, Grain,Ethyl Alcohol
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000897 Anti-Ulcer Agents Various agents with different action mechanisms used to treat or ameliorate PEPTIC ULCER or irritation of the gastrointestinal tract. This has included ANTIBIOTICS to treat HELICOBACTER INFECTIONS; HISTAMINE H2 ANTAGONISTS to reduce GASTRIC ACID secretion; and ANTACIDS for symptomatic relief. Anti-Ulcer Drugs,Agents, Anti-Ulcer,Anti Ulcer Agents,Anti Ulcer Drugs,Drugs, Anti-Ulcer
D001285 Atropine An alkaloid, originally from Atropa belladonna, but found in other plants, mainly SOLANACEAE. Hyoscyamine is the 3(S)-endo isomer of atropine. AtroPen,Atropin Augenöl,Atropine Sulfate,Atropine Sulfate Anhydrous,Atropinol,Anhydrous, Atropine Sulfate,Augenöl, Atropin,Sulfate Anhydrous, Atropine,Sulfate, Atropine
D013276 Stomach Ulcer Ulceration of the GASTRIC MUCOSA due to contact with GASTRIC JUICE. It is often associated with HELICOBACTER PYLORI infection or consumption of nonsteroidal anti-inflammatory drugs (NSAIDS). Gastric Ulcer,Gastric Ulcers,Stomach Ulcers,Ulcer, Gastric,Ulcer, Stomach,Ulcers, Gastric,Ulcers, Stomach
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships

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