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N(G)-Acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent

Igel, Patrick and Schneider, Erich and Schnell, David and Elz, Sigurd and Seifert, Roland and Buschauer, Armin (2009) N(G)-Acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent. Journal of Medicinal Chemistry 52 (8), pp. 2623-2627.

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Abstract

3-(1H-imidazol-4-yl)propylguanidine (SK&F 91486, 4) was identified as a potent partial agonist at the human histamine H3 receptor (hH3R) and human histamine H4 receptor (hH4R). With the aim to increase selectivity for the hH4R, the guanidine group in 4 was acylated. N1-Acetyl-N2-[3-(1H-imidazol-4-yl)propyl]guanidine (UR-PI288, 13) was a potent full agonist at hH4R (pEC50: 8.31, α: 1.00), ...

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Item Type:Article
Date:24 March 2009
Additional information (public):Supplementary Material available at http:// pubs.acs.org
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Chemistry and Pharmacy > Institute of Pharmacy > Pharmacology and Toxicology (Prof. Schlossmann formerly Prof. Seifert)
Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz)
Projects:GRK 760, Graduiertenkolleg Medizinische Chemie
Identification Number:
ValueType
10.1021/jm9000693DOI
19317445PubMed ID
Related URLs:
URLURL Type
http://pubs.acs.org/doi/pdf/10.1021/jm9000693Publisher
http://pubs.acs.org/doi/suppl/10.1021/jm9000693/suppl_file/jm9000693_si_001.pdfSupplementary Material
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:09 Mar 2009 14:07
Last Modified:05 Aug 2009 13:48
Item ID:4923
Owner Only: item control page
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