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ChemInform Abstract: Nicotinamide Derivatives as a New Class of Gastric H+/K+-ATPase Inhibitors. Part 1. Synthesis and Structure-Activity Relationships of N-Substituted 2-(Benzhydryl- and benzylsulfinyl)nicotinamides.

✍ Scribed by H. TERAUCHI; A. TANITAME; K. TADA; K. NAKAMURA; Y. SETO; Y. NISHIKAWA

Publisher
John Wiley and Sons
Year
2010
Weight
35 KB
Volume
28
Category
Article
ISSN
0931-7597

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✦ Synopsis

Nicotinamide Derivatives as a New Class of Gastric H+/K+-ATPase Inhibitors. Part 1. Synthesis and Structure-Activity Relationships of N-Substituted 2-(Benzhydryl-and benzylsulfinyl)nicotinamides.

-A series of title compounds, e.g. (IV), (VIII), (IX), and (X), is synthesized. Acid activation converts them into their active isothiazolopyridine form. In comparison to reference compound omeprazole (XI), nicotinamide (Xa) possesses equivalent inhibitory activities in vitro and in vivo, is much more stable at neutral and weakly acidic pH and, thus, is a promising agent for treating acid-related gastrointestinal disorders. -(TERAUCHI, H.; TANITAME, A.;

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