Abstract：
:Naturally occurring polyamines: putrescine, spermidine and spermine are crucial for Kinetoplastid growth and persistence. These aliphatic polycations are either biosynthesized or internalized into Kinetoplastid by active transport. Impairing the polyamine metabolism using polyamine derivatives is an interesting path in the search of new antikinetoplastid chemotherapy. In the past 30 years, research interest in this field has been constantly expanding and recent results demonstrated that the discovery of a polyamine-based antikinetoplastid drug is undoubtedly possible. In this paper, all the polyamine derivatives previously described to present an antikinetoplastid activity are reported. This review is organized around three main parts which are diamine, triamine and tetramine derivatives. Each part includes the description of the series of molecules and, their in vitro and in vivo activity when available. Structure-activity relationships of these derivatives are discussed and the most promising structures for a positive outcome are eventually highlighted.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Jagu E,Pomel S,Pethe S,Loiseau PM,Labruère Rdoi
10.1016/j.ejmech.2017.08.014subject
Has Abstractpub_date
2017-10-20 00:00:00pages
982-1015eissn
0223-5234issn
1768-3254pii
S0223-5234(17)30617-7journal_volume
139pub_type
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journal_title：European journal of medicinal chemistry
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journal_title：European journal of medicinal chemistry
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