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Acylguanidines as bioisosteric groups in argininamide-type neuropeptide Y Y1 and Y2 receptor antagonists: synthesis, stability and pharmacological activity

URN to cite this document: urn:nbn:de:bvb:355-opus-7423

Brennauer, Albert (2006) Acylguanidines as bioisosteric groups in argininamide-type neuropeptide Y Y1 and Y2 receptor antagonists: synthesis, stability and pharmacological activity. PhD, Universität Regensburg

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Abstract (English)

We developed multi-step synthetic routes for the preparation of two classes of N(G)-substituted argininamides with neuropeptide Y Y1 and Y2 receptor selective antagonistic activity, respectively. In both series we could identify N(G)-acylated analogs being even more potent than the respective N(G)-unsubstituted compounds, which are established as standard Y1- (BIBP 3226) and Y2-antagonists (BIIE ...

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Translation of the abstract (German)

Wir beschäftigten uns mit der Synthese von zwei verschiedenen Klassen von N(G)-substituierten Argininamiden mit Neuropeptid Y Y1- bzw. Y2-rezeptorselektiver antagonistischer Wirkung. In beiden Serien fanden sich N(G)-acylierte Analogverbindungen, die potenter sind als die entsprechenden unsubstituierten Verbindungen BIBP 3226 und BIIE 0246, die als Standard Y1- bzw. Y2-Rezeptorantagonisten in der ...

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Item Type:Thesis of the University of Regensburg (PhD)
Date:14 December 2006
Referee:Prof. Dr. Armin Buschauer
Date of exam:11 September 2006
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Keywords:Neuropeptid Y , Pharmakologischer Antagonist , Argininderivate , Guanidinderivate , Peptidomimetikum , Organische Synthese , Amide , Chemische Synthese , Rezeptor , NPY Rezeptoren , Y1 Rezeptor , Y2 Rezeptor , BIBP 3226 , BIIE 0246 , Guanidinylierung , NPY receptors , Y1 receptor , Y2 receptor , BIBP 3226 , BIIE 0246 , guanidinylation
Subjects:500 Science > 540 Chemistry & allied sciences
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Owner: Universitätsbibliothek Regensburg
Deposited On:27 Oct 2009 07:52
Last Modified:13 Mar 2014 11:41
Item ID:10487
Owner Only: item control page

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