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Article

The bivalent ligand approach leads to highly potent and selective acylguanidine-type histamine H₂ receptor agonists.

Journal of medicinal chemistry - 9 Feb 2012

Birnkammer Tobias, Spickenreither Anja, Brunskole Irena, Lopuch Miroslaw, Kagermeier Nicole, Bernhardt Günther, Dove Stefan, Seifert Roland, Elz Sigurd, Buschauer Armin

Abstract excerpt

Bivalent histamine H(2) receptor (H(2)R) agonists were synthesized by connecting pharmacophoric 3-(2-amino-4-methylthiazol-5-yl)-, 3-(2-aminothiazol-5-yl)-, 3-(imidazol-4-yl)-, or 3-(1,2,4-triazol-5-yl)propylguanidine moieties by N(G)-acylation with alkanedioic acids of various chain lengths. The compounds were investigated for H(2)R agonism in GTPase and [(35)S]GTPγS binding assays at guinea pig (gp) and human...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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PMID: 22216892
DOI: 10.1021/jm201128q

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