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Conformational restriction and enantioseparation increase potency and selectivity of cyanoguanidine-type histamine H4 receptor agonists

Geyer, Roland, Nordemann, Uwe, Strasser, Andrea, Wittmann, Hans-Joachim and Buschauer, Armin (2016) Conformational restriction and enantioseparation increase potency and selectivity of cyanoguanidine-type histamine H4 receptor agonists. Journal of Medicinal Chemistry 59 (7), pp. 3452-3470.

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Abstract

2-Cyano-1-[4-(1H-imidazol-4-yl)butyl]-3-[2-(phenylsulfanyl)ethyl]guanidine (UR-PI376, 1) is a potent and selective agonist of the human histamine H4 receptor (hH4R). To gain information on the active conformation, we synthesized analogues of 1 with a cyclopentane-1,3-diyl linker. Affinities and functional activities were determined at recombinant hHxR (x: 1-4) subtypes on Sf9 cell membranes ...

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Item type:Article
Date:23 March 2016
Additional Information (public):Supplementary Material available online
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Projects:GRK 1910, Graduiertenkolleg "Medicinal Chemistry of Selective GPCR Ligands", GRK 760, Graduiertenkolleg Medizinische Chemie
Identification Number:
ValueType
10.1021/acs.jmedchem.6b00120DOI
27007611PubMed ID
Keywords:Conformational restriction, Cyanoguanidine, Histamine H4 receptor, (1S,3S)-UR-RG98, UR-PI376, Molecular dynamics, chiral discrimination
Dewey Decimal Classification:600 Technology > 615 Pharmacy
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Item ID:33233
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