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

Birnkammer, Tobias, Spickenreither, Anja, Brunskole, Irena, Lopuch, Miroslaw, Kagermeier, Nicole, Bernhardt, Günther, Dove, Stefan, Seifert, Roland, Elz, Sigurd und Buschauer, Armin (2012) The bivalent ligand approach leads to highly potent and selective acylguanidine-type histamine H2 receptor agonists. Journal of Medicinal Chemistry 55 (3), S. 1147-1160.

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Andere URL zum Volltext: http://pubs.acs.org/doi/pdf/10.1021/jm201128q

Zusammenfassung

Bivalent histamine H2 receptor (H2R) 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 NG-acylation with alkanedioic acids of various chain lengths. The compounds were investigated for H2R agonism in GTPase and [35S]GTPγS binding assays at guinea pig (gp) and ...

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