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

Birnkammer, Tobias and Spickenreither, Anja and Brunskole, Irena and Lopuch, Miroslaw and Kagermeier, Nicole and Bernhardt, Günther and Dove, Stefan and Seifert, Roland and Elz, Sigurd and 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), pp. 1147-1160.

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Other URL: http://pubs.acs.org/doi/pdf/10.1021/jm201128q


Abstract

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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Item Type:Article
Date:5 January 2012
Additional information (public):Online veröffentlicht als "just accepted manuscript" am 5. Januar 2012
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz)
Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Projects:GRK 760, Graduiertenkolleg Medizinische Chemie
Research groups and research centres:Not selected
Identification Number:
ValueType
10.1021/jm201128qDOI
22216892PubMed ID
Related URLs:
URLURL Type
http://pubs.acs.org/doi/suppl/10.1021/jm201128q/suppl_file/jm201128q_si_001.pdfSupplementary Material
Keywords:Acylguanidine, bivalent ligand, GTPase assay, histamine H2 receptor, receptor selectivity
Subjects:500 Science > 540 Chemistry & allied sciences
500 Science > 570 Life sciences
600 Technology > 615 Pharmacy
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Owner: Prof. Armin Buschauer
Deposited On:09 Jan 2012 12:23
Last Modified:07 Jul 2012 07:38
Item ID:21744
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