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2-[(2-Pyridylmethyl)sulfinyl]-1H-thieno[3,4-d]imidazoles. A novel class of gastric H+/K+-ATPase inhibitors

Weidmann, Klaus ; Herling, Andreas W ; Lang, Hans Jochen ; Scheunemann, Karl Heinz ; Rippel, Robert ; Nimmesgern, Hildegard ; Scholl, Thomas ; Bickel, Martin ; Metzger, Heinz

Journal of medicinal chemistry, 1992-02, Vol.35 (3), p.438-450 [Periódico revisado por pares]

Washington, DC: American Chemical Society

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2-[(2-Pyridylmethyl)sulfinyl]-1H-thieno[3,4-d]imidazoles. A novel class of gastric H+/K+-ATPase inhibitors
Autor: Weidmann, Klaus ; Herling, Andreas W ; Lang, Hans Jochen ; Scheunemann, Karl Heinz ; Rippel, Robert ; Nimmesgern, Hildegard ; Scholl, Thomas ; Bickel, Martin ; Metzger, Heinz
Assuntos: Animals ; Chemistry ; Dogs ; Enzyme Inhibitors - chemical synthesis ; Enzyme Inhibitors - pharmacology ; Exact sciences and technology ; Female ; Heterocyclic compounds ; Heterocyclic compounds with n hetero atom and also o and/or s, se, te hetero atoms ; Imidazoles - chemical synthesis ; Imidazoles - pharmacology ; Male ; Omeprazole - pharmacology ; Organic chemistry ; Preparations and properties ; Rats ; Rats, Inbred Strains ; Sodium-Potassium-Exchanging ATPase - antagonists & inhibitors ; Stomach - enzymology ; Structure-Activity Relationship
É parte de: Journal of medicinal chemistry, 1992-02, Vol.35 (3), p.438-450
Notas: istex:4150A93C340E2E5B942A8DA0FA00DC00E96D3109
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ObjectType-Article-1
SourceType-Scholarly Journals-1
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Descrição: 2-[(2-Pyridylmethyl)sulfinyl]thienoimidazoles were synthesized and investigated as potential inhibitors of gastric H+/K(+)-ATPase. The [3,4-d] isomers of the two possible thienoimidazole series were found to be potent inhibitors of gastric acid secretion in vitro and in vivo. Structure-activity relationships indicate that especially lipophilic alkoxy, benzyloxy, and phenoxy substituents with additional electron-demanding properties in the 4-position of the pyridine moiety combined with an unsubstituted thieno[3,4-d]imidazole lead to highly active compounds with a favorable chemical stability. Various substitution patterns in the thieno[3,4-d]imidazole moiety result in lower biological activity. The heptafluorobutyloxy derivative saviprazole (HOE 731, 5d) was selected for further development and is currently undergoing clinical evaluation. Comprehensive pharmacological studies indicate a pharmacodynamic profile different to omeprazole, the first H+/K(+)-ATPase blocker introduced on the market.
Editor: Washington, DC: American Chemical Society
Idioma: Inglês

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2-[(2-Pyridylmethyl)sulfinyl]-1H-thieno[3,4-d]imidazoles. A novel class of gastric H+/K+-ATPase inhibitors

Weidmann, Klaus ; Herling, Andreas W ; Lang, Hans Jochen ; Scheunemann, Karl Heinz ; Rippel, Robert ; Nimmesgern, Hildegard ; Scholl, Thomas ; Bickel, Martin ; Metzger, Heinz

Washington, DC: American Chemical Society

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