- Method of reducing blood pressure
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Disclosed is a method of reducing blood pressure which comprises administering to a patient an imidazole derivative of the formula: STR1 wherein: each of R1 and R2 is hydrogen, substituted or unsubstituted alkyl, alkoxyalkyl, cycloalkyl, aryl, aralkyl, or R1 and R2 are combined to form hetero ring; each of R3, R4, R5 and R6 is hydrogen, halogen, substituted or unsubstituted alkoxy, substituted or unsubstituted alkyl, aryl, aryloxy, alkoxycarbonyl, nitro, amino, acyl, or R3 is combined with R2 to form heteroring; R7 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylcarbonyl, or S-containing heteroring; each of R8 and R9 is hydrogen, halogen, substituted or unsubstituted alkoxy, unsubstituted or substituted alkyl, alkoxycarbonyl, aralkyl, nitro, amino, acyl, substituted or unsubstituted aryl, or R8 and R9 are combined to from alkylene; and n is 0 or 1.
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- Anti-ulcer composition containing imidazole derivative
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Disclosed is an anti-ulcer composition to be dissolved in stomach to become directly into contact with walls of the stomach which comprises 100 weight parts of an imidazole derivative of the formula: wherein each of R1 and R2 is hydrogen, substituted or unsubstituted alkyl, alkoxyalkyl, cycloalkyl, aryl, aralkyl, or R1 and R2 are combined to form hetero ring; each of R3, R4, R5 and R6 is hydrogen, halogen, substituted or unsubstituted alkoxy, substituted or unsubstituted alkyl, aryl, aryloxy, alkoxycarbonyl, nitro, amino, acyl, or R3 is combined with R2 to form heteroring; R7 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylcarbonyl, or S-containing heteroring; and each of R8 and R9 is hydrogen, halogen, substituted or unsubstituted alkoxy, unsubstituted or substituted alkyl, alkoxycarbonyl, aralkyl, nitro, amino, acyl, substituted or unsubstituted aryl, or R8 and R9 are combined to form alkylene, and 50 - 2,000 weigt parts of a basic material.
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- Novel imidazole derivatives
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Disclosed are novel imidazole derivatives having the formula: STR1 wherein R1 and R2 are H, alkyl, cycloalkyl, aryl, aralkyl or halogen-substituted alkyl, or R1 and R2 are combined to form a heterocyclic ring; R3, R4, R5 and R6 are H, halogen, alkoxy, aralkyloxy, alkyl, alkoxycarbonyl, nitro, amino, acyl, fluorine substituted-alkyl, or fluorine substituted-alkoxy, or R3 is combined with R2 to form a heterocyclic ring; R8 and R9 are H, halogen, alkoxy, alkyl, alkoxycarbonyl, nitro, amino, acyl, fluorine substituted-alkyl, fluorine substituted-alkoxy, or aryl group which may have a substituent, or R8 and R9 are combined to form an alicyclic ring; R7 is, where R8 and R9 are not combined, H, and, where R8 and R9 are combined, H, alkyl which may have a substituent, aryl which may have a substituent, arylcarbonyl which may have a substituent, or a sulfur-containing heterocyclic group; and n is 0 or 1. The new imidazole derivatives are effective particularly as anti-ulcer agents.
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- Synthesis and structure-activity relationships of N-substituted 2-[(2-imidazolylsulfinyl)methyl]anilines as a new class of gastric H+/K+-ATPase inhibitors
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A series of N-substituted 2-[(2-imidazolylsulfinyl)methyl]anilines was synthesized and evaluated for its biological activity against H+/K+-ATPase prepared from rabbit stomach and gastric acid secretions in Heidenhain pouch dogs. Monoalkyl substituents on the nitrogen atom of the aniline moiety markedly inhibited the enzyme activity to the same degree as omeprazole, a representative H+/K+-ATPase inhibitor. Most of these compounds, administered at 3 mg/kg i.v. inhibited histamine-stimulated gastric acid secretion. The inhibitory activity of these derivatives on the enzymes at pH 6.0 was more potent than that at pH 7.4, and was distinctly correlated to stability in aqueous solution at pH 5.0.
- Yamakawa,Matsukura,Nomura,Yoshioka,Masaki,Igata,Okabe
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p. 1746 - 1752
(2007/10/02)
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