Patil, Rameshwar and Elz, Sigurd and Reiser, Oliver (2006) Side-chain modified analogues of histaprodifen: Asymmetric synthesis and histamine H-1-receptor activity. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 16 (3). pp. 672-676. ISSN 0960-894X, 1464-3405
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New analogues of histaprodifen with polar side chains have been stereo selectively synthesized and evaluated as histamine H-1-receptor agonists. As a key transformation the asymmetric aminohydroxylation has been used, which was successfully realized for the first time on an imidazolyl derivative. While all chiral analogues proved to be weak H-1-receptor antagonists, an achiral keto derivative of histaprodifen turned out to be the first 2-acylated histamine congener displaying partial H-1-receptor agonism (relative potency 12%). (c) 2005 Elsevier Ltd. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | HETEROAROMATIC ACRYLATES; AMINOHYDROXYLATION; AGONISTS; histamine; histaprodifen; asymmetric aminohydroxylation; urocanic acids; imidazole |
| Subjects: | 500 Science > 540 Chemistry & allied sciences 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz) Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Oliver Reiser |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 24 Feb 2021 05:53 |
| Last Modified: | 24 Feb 2021 05:53 |
| URI: | https://pred.uni-regensburg.de/id/eprint/34967 |
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