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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