115198-80-6Relevant articles and documents
Selective delivery of 2-hydroxy APA to Trypanosoma brucei using the melamine motif
Klee, Nina,Wong, Pui Ee,Baragana, Beatriz,Mazouni, Farah El,Phillips, Margaret A.,Barrett, Michael P.,Gilbert, Ian H.
, p. 4364 - 4366 (2010)
Trypanosoma brucei, the parasite that causes human African trypanosomiasis, is auxotrophic for purines and has specialist nucleoside transporters to import these metabolites. In particular, the P2 aminopurine transporter can also selectively accumulate melamine derivatives. In this Letter, we report the coupling of the melamine moiety to 2-hydroxy APA, a potent ornithine decarboxylase inhibitor, with the aim of selectively delivering this compound to the parasite. The best compound described here shows an increased in vitro trypanocidal activity compared with the parent.
BISPHOSPHONATE-LINKED COMPOUNDS
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Page/Page column 21, (2020/08/22)
The present invention concerns novel compounds useful in the treatment of cancer, particularly including compounds linking a bisphosphonate moiety with KBU2046, and pharmaceutically acceptable salts, co-crystals, polymorphs, solvates, hydrates, and enantiomers thereof, as well as methods for their production and pharmaceutical compositions comprising them.
TGR5 AGONISTS
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, (2016/10/24)
The invention relates to novel 1,4-diazepan-2-one compounds, which are TGR5 agonists and useful for the treatment of metabolic disorders, inflammatory diseases, atherosclerosis and dyslipidemias.