Birnkammer, Tobias, Spickenreither, Anja, Brunskole, Irena, Lopuch, Miroslaw, Kagermeier, Nicole, Bernhardt, Günther, Dove, Stefan, Seifert, Roland, 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 | ||||||
| Interdisciplinary Subject Network: | Not selected | ||||||
| Identification Number: |
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| Keywords: | Acylguanidine, bivalent ligand, GTPase assay, histamine H2 receptor, receptor selectivity | ||||||
| Dewey Decimal Classification: | 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 | ||||||
| Item ID: | 21744 |
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