Patil, Rameshwar and Elz, Sigurd and Reiser, Oliver (2006) Side-chain modified analogues of histaprodifen: Asymmetric synthesis and histamine H₁-receptor activity. Bioorg. Med. Chem. Lett. 16 (3), pp. 672-676.
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Other URL: http://dx.doi.org/10.1016/j.bmcl.2005.10.030
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%).
|Date:||1 February 2006|
|Institutions:||Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Oliver Reiser|
|Subjects:||500 Science > 540 Chemistry & allied sciences|
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Yes|
|Owner:||Helge Knüttel (ADMIN)|
|Deposited On:||05 Sep 2006|
|Last Modified:||05 Aug 2009 13:22|