Add time:08/01/2019         Source:sciencedirect.com

Structure-activity relationships for a series of 65 H2-agonists of the impromidine (phenyl analogues) and arpromidine type were investigated by Free-Wilson analysis. These compounds have in common an imidazolylpropylguanidine moiety which is connected to 1 or 2 aromatic rings through a flexible aliphatic chain which may or may not contain heteroatoms. In one of the rings, substituents are varied in all positions. Free-Wilson analysis revealed that the properties of the side chain and the arrangement of rings are of primary importance for receptor affinity, while substituents showed an irregular pattern of only marginal contributions. The latter is due to the fact that substituent effects are not constant but vary with changes in the chain. This could be verified in a second analysis after introducing appropriate interaction parameters.

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