Ghorai, Prasanta and Kraus, Anja and Birnkammer, Tobias and Geyer, Roland and Bernhardt, Guenther and Dove, Stefan and Seifert, Roland and Elz, Sigurd and Buschauer, Armin (2010) Chiral N-G-acylated hetarylpropylguanidine-type histamine H-2 receptor agonists do not show significant stereoselectivity. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 20 (10). pp. 3173-3176. ISSN 0960-894X,
Full text not available from this repository. (Request a copy)Abstract
A set of chiral imidazolylpropylguanidines and 2-aminothiazolylpropylguanidines bearing N-G-3-phenyl- or N-G-3-cyclohexylbutanoyl residues was synthesized and investigated for histamine H-2 receptor (H2R) agonism ( guinea pig (gp) right atrium, GTPase assay on recombinant gp and human (h)H2R) and for hH(2)R selectivity compared to hH(1)R, hH(3)R and hH(4)R. In contrast to previous studies on arpromidine derivatives, the present investigation of acylguanidine-type compounds revealed only very low eudismic ratios (1.1-3.2), indicating the stereochemistry of the acyl moiety to play only a minor role in this series of H2R agonists. (C) 2010 Elsevier Ltd. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | CONJUGATE ADDITIONS; POTENT; IMIDAZOLYLPROPYLGUANIDINES; H-1-RECEPTOR; PHARMACOLOGY; AUXILIARIES; SELECTIVITY; GUANIDINES; H-3; Histamine; H-2 receptor agonist; Chiral; Enantiomers; Acylguanidine; Sf9 cells |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz) Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 30 Jul 2020 10:38 |
| Last Modified: | 30 Jul 2020 10:38 |
| URI: | https://pred.uni-regensburg.de/id/eprint/24724 |
Actions (login required)
 |
View Item |
