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N(G)-Acylated aminothiazolylpropylguanidines as potent and selective histamine H2 receptor agonists

Kraus, Anja ; Ghorai, Prasanta ; Birnkammer, Tobias ; Schnell, David ; Elz, Sigurd ; Seifert, Roland ; Dove, Stefan ; Bernhardt, Günther ; Buschauer, Armin


The bioisosteric replacement of the guanidino group in arpromidine-like histamine H2 receptor (H2R) agonists by an acylguanidine moiety is a useful approach to obtain potent H2R agonists with improved oral bioavailability and penetration across the blood brain barrier. Unfortunately, the selectivity of such N(G)-acylated imidazolylpropyl-guanidines for the H2R is poor, in particular versus ...


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