Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines.
نویسندگان
چکیده
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.
منابع مشابه
Synthesis and characterization of new (2E,2'E)-3,3'-(((3-hydroxypropane-1,2-diyl)bis(oxy))bis (2,1-phenylene))bis(1-phenylprop-2-en-1-one) and its transformation into 2,3-bis(2-(1,3-diphenyl-4,5-dihydro-1H-pyrazol-5-yl)phenoxy)propan-1-ol
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ورودعنوان ژورنال:
- Bioorganic & medicinal chemistry letters
دوره 24 23 شماره
صفحات -
تاریخ انتشار 2014