Abstract：
:A novel one-pot synthesis of tri-substituted purines and the discovery of purine analogues with trypanocidal activity are reported. The reaction is initiated by a metal-free oxidative coupling of primary alkoxides and diaminopyrimidines with Schiff base formation and subsequent annulation in the presence of large N,N-dimethylamides (e.g. N,N-dimethylpropanamide or larger). This synthetic route is in competition with a reaction previously-reported by our group, allowing the generation of a combinatorial library of tri-substituted purines by the simple modification of the amide and the alkoxide employed. Among the variety of structures generated, two purine analogues displayed trypanocidal activity against the protozoan parasite Trypanosoma brucei with IC50 < 5 μM, being each of those compounds obtained through each of the synthetic pathways.
journal_name
Sci Repjournal_title
Scientific reportsauthors
Pineda de las Infantas y Villatoro MJ,Unciti-Broceta JD,Contreras-Montoya R,Garcia-Salcedo JA,Gallo Mezo MA,Unciti-Broceta A,Diaz-Mochon JJdoi
10.1038/srep09139subject
Has Abstractpub_date
2015-03-16 00:00:00pages
9139issn
2045-2322pii
srep09139journal_volume
5pub_type
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