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|Title: ||Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines|
|Authors: ||Sola, Irene|
Taylor, Martin C.
Gbedema, Stephen Y.
Clos, M. Victòria
Wright, Colin W.
Kelly, John M.
|Keywords: ||Molecular dimerization|
|Issue Date: ||2014|
|Publisher: ||Bioorganic & Medicinal Chemistry Letters|
|Citation: ||Bioorganic & Medicinal Chemistry Letters 24 (2014) 5435–5438|
|Abstract: ||We have synthesized a series of dimers of (+)-(7R,11R)-huprine Y and evaluated their activity against
Trypanosoma brucei, Plasmodium falciparum, rat myoblast L6 cells and human acetylcholinesterase
(hAChE), and their brain permeability. Most dimers have more potent and selective trypanocidal activity
than huprine Y and are brain permeable, but they are devoid of antimalarial activity and remain active
against hAChE. Lead optimization will focus on identifying compounds with a more favourable trypanocidal/
anticholinesterase activity ratio.|
|Description: ||An article published by Bioorganic & Medicinal Chemistry Letters 24 (2014) 5435–5438|
|Appears in Collections:||College of Health Sciences|
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