SAR of H2-receptor Antagonists

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Chapter: Medicinal Chemistry : Antiulcer Agents

The H2-receptor antagonists were the result of the international modification of the histamine structure and deliberate search for a chemically related substance that would act as competitive inhibitor of the H2-receptors.


SAR of H2-receptor Antagonists

The H2-receptor antagonists were the result of the international modification of the histamine structure and deliberate search for a chemically related substance that would act as competitive inhibitor of the H2-receptors.


·Imidazole ring is not the only required ring for competitive antagonism of histamine H2 -receptors.

·Other heterocyclic rings (furan, thiophene, thiazole, etc) that enhance the potency and selectivity of H2-receptor antagonism can be used.

·The ring and terminal nitrogen should be separated by four carbon atoms for optimum antagonistic activity. The isosteric thioether link is also present in certain drugs.

·The terminal nitrogen group should be polar, nonbasic substituents for maximal antagonist activity.

In general, antagonistic activity varies inversely with the hydrophilic character of the nitrogen group (exception ranitidine and nizatidine)

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