Abstract
A series of 6-[2-(imidazo[1,2-a]pyridin-2-yl)ethyl]benzothiazoles (II) and benzimidazole analogues (III) was synthesized and tested for histamine H2-receptor antagonist, gastric antisecretory and anti-stress ulcer activity. A benzimidazole derivative (IIIa) exhibited strong antisecretory activity, whereas the corresponding benzothiazole derivative (IIb) lacked this potency in in vivo test. In contrast to compound IIIa, however, compound IIb demonstrated good inhibition against stress induced ulcer. The structure-activity relationships of these compounds are discussed.
MeSH terms
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Animals
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Anti-Ulcer Agents / chemical synthesis*
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Anti-Ulcer Agents / pharmacology
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Benzimidazoles / chemical synthesis*
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Benzimidazoles / pharmacology
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Guinea Pigs
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Histamine H2 Antagonists / chemical synthesis*
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Histamine H2 Antagonists / pharmacology
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In Vitro Techniques
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Pyridines / chemical synthesis*
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Pyridines / pharmacology
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Rabbits
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Stomach Ulcer / chemically induced
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Stomach Ulcer / prevention & control*
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Stress, Psychological / complications
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Thiazoles / chemical synthesis*
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Thiazoles / pharmacology
Substances
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Anti-Ulcer Agents
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Benzimidazoles
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Histamine H2 Antagonists
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Pyridines
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Thiazoles