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Chiral N(G)-acylated hetarylpropylguanidine-type histamine H2 receptor agonists do not show significant stereoselectivity

Ghorai, Prasanta and Kraus, Anja and Birnkammer, Tobias and Geyer, Roland and Bernhardt, Günther and Dove, Stefan and Seifert, Roland and Elz, Sigurd and Buschauer, Armin (2010) Chiral N(G)-acylated hetarylpropylguanidine-type histamine H2 receptor agonists do not show significant stereoselectivity. Bioorganic & Medicinal Chemistry Letters 20 (10), pp. 3173-3176.

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Abstract

A set of chiral imidazolylpropylguanidines and 2-aminothiazolylpropylguanidines bearing N(G)-3-phenyl- or N(G)-3-cyclohexylbutanoyl residues was synthesized and investigated for histamine H2 receptor (H2R) agonism (guinea pig (gp) right atrium, GTPase assay on recombinant gp and human (h) H2R) and for hH2R selectivity compared to hH1R, hH3R and hH4R. In contrast to previous studies on arpromidine ...

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Item Type:Article
Date:27 March 2010
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz)
Projects:GRK 760, Graduiertenkolleg Medizinische Chemie
Identification Number:
ValueType
10.1016/j.bmcl.2010.03.082DOI
20409707PubMed ID
Related URLs:
URLURL Type
http://www.sciencedirect.com/science/MiamiMultiMediaURL/B6TF9-4YPPPY3-4/B6TF9-4YPPPY3-4-9/5221/html/S0960894X10004130/838bbb3db83fce38f96e20eff3be8934/mmc1.pdfSupplementary Material
Keywords:histamine; H2 receptor agonist; chiral; enantiomers; acylguanidine; Sf9 cells
Subjects:500 Science > 570 Life sciences
500 Science > 540 Chemistry & allied sciences
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Owner: Prof. Armin Buschauer
Deposited On:26 Mar 2010 10:16
Last Modified:01 May 2010 07:00
Item ID:13775
Owner Only: item control page
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