| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1367645 | Bioorganic & Medicinal Chemistry Letters | 2006 | 5 Pages |
Abstract
New analogues of histaprodifen with polar side chains have been stereoselectively synthesized and evaluated as histamine H1-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 H1-receptor antagonists, an achiral keto derivative of histaprodifen turned out to be the first 2-acylated histamine congener displaying partial H1-receptor agonism (relative potency 12%).
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Rameshwar Patil, Sigurd Elz, Oliver Reiser,