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2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor - H1/H4-receptor selectivity

Hammer, Sebastian, Gobleder, Susanne, Naporra, Franziska, Wittmann, Hans-Joachim, Elz, Sigurd, Heinrich, Markus and Strasser, Andrea (2016) 2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor - H1/H4-receptor selectivity. Bioorganic & Medicinal Chemistry Letters 26, pp. 292-300.

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Abstract

Distinct diaminopyrimidines, for example, 4-(4-methylpiperazin-1-yl)-5,6-dihydrobenzo[h]quinazolin-2-amine are histamine H4 receptor (H4R) antagonists and show high affinity to the H4R, but only a moderate affinity to the histamine H1 receptor (H1R). Within previous studies it was shown that an aromatic side chain with a distinct distance to the basic amine and aromatic core is necessary for ...

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Item type:Article
Date:2016
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)
Identification Number:
ValueType
10.1016/j.bmcl.2015.12.035DOI
Keywords:Histamine H1 receptor; Histamine H4 receptor; Diaminopyrimidines; Dual H1R/H4R ligands; Molecular dynamics
Dewey Decimal Classification:600 Technology > 615 Pharmacy
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Partially
Item ID:33119
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