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Imidazolylpropylguanidines as histamine H_2 receptor agonists: 3D-QSAR of a large series

Dove, Stefan ; Buschauer, Armin



Abstract

Imidazolylpropylguanidines are potent histamine H2 receptor agonists and act as inotropic vasodilators. A large series of 141 derivatives was tested in the isolated guinea pig atrium and submitted to CoMFA. Since all compounds are full agonists, pD2 values reflect H2 receptor binding. Hydrophobicity was considered as Σf of the variable structural moiety, calculated by the Leo–Hansch method. ...

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