| Title : Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines - Sola_2014_Bioorg.Med.Chem.Lett_24_5435 |
| Author(s) : Sola I , Artigas A , Taylor MC , Gbedema SY , Perez B , Clos MV , Wright CW , Kelly JM , Munoz-Torrero D |
| Ref : Bioorganic & Medicinal Chemistry Lett , 24 :5435 , 2014 |
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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. |
| PubMedSearch : Sola_2014_Bioorg.Med.Chem.Lett_24_5435 |
| PubMedID: 25454267 |
Sola I, Artigas A, Taylor MC, Gbedema SY, Perez B, Clos MV, Wright CW, Kelly JM, Munoz-Torrero D (2014)
Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines
Bioorganic & Medicinal Chemistry Lett
24 :5435
Sola I, Artigas A, Taylor MC, Gbedema SY, Perez B, Clos MV, Wright CW, Kelly JM, Munoz-Torrero D (2014)
Bioorganic & Medicinal Chemistry Lett
24 :5435