Geyer, Roland and Igel, Patrick and Kaske, Melanie and Elz, Sigurd and Buschauer, Armin (2014) Synthesis, SAR and selectivity of 2-acyl-and 2-cyano-1-hetarylalkyl-guanidines at the four histamine receptor subtypes: a bioisosteric approach. MEDCHEMCOMM, 5 (1). pp. 72-81. ISSN 2040-2503, 2040-2511
Full text not available from this repository. (Request a copy)Abstract
In the search for potential bioisosteres of the 4-imidazolyl ring in acylguanidines (e. g. UR-AK24), known to possess affinity to several histamine receptor subtypes (HxR, x = 1-4), and cyanoguanidine- type H4R agonists (e. g. UR-PI376), the contribution of various heterocycles to agonism, antagonism and HR subtype selectivity was studied (recombinant human H(1,2,3,4)Rs, isolated guinea pig organs (H1R, H2R)). While minor structural modifications of UR- PI376 analogues were not tolerated regarding H4R agonism, in the case of the acylguanidines, a 1,2,4-triazole ring shifted the selectivity toward the H2R.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | G-ACYLATED IMIDAZOLYLPROPYLGUANIDINES; H-4 RECEPTOR; GUINEA-PIG; GUANOSINE 5-O-(3-THIOTRIPHOSPHATE); PHARMACOLOGICAL CHARACTERIZATION; STIMULATED BINDING; MOLECULAR-CLONING; 1ST POTENT; H-2-RECEPTOR; H-1-RECEPTOR; |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz) Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 02 Dec 2019 10:19 |
| Last Modified: | 02 Dec 2019 10:19 |
| URI: | https://pred.uni-regensburg.de/id/eprint/11108 |
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