@misc{10481/35509,
year = {2015},
url = {http://hdl.handle.net/10481/35509},
abstract = {Anovel 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 group1, 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 mM, being each of those compounds obtained through each of the synthetic pathways.},
organization = {J.J.D.M. thanks Spanish Ministerio de Economı´a y Competitividad for a Ramon y Cajal
Fellowship. A.U.B. thanks MRC IGMM for an academic fellowship. This work was partially
supported by Grant SAF2011-30528 to J.A.G.S..},
publisher = {Nature Publishing Group},
keywords = {Reaction mechanisms},
keywords = {Parasite biology},
keywords = {Purines},
keywords = {Trypanosoma brucei},
keywords = {Trypanocidal activity},
title = {Amide-controlled, one-pot synthesis of tri-substituted purines generates structural diversity and analogues with trypanocidal activity},
doi = {10.1038/srep09139},
author = {Pineda de las Infantas y Villatoro, María J. and Unciti-Broceta, Juan Diego and Contreras-Montoya, Rafael and García-Salcedo, José Antonio and Gallo Mezo, Miguel Ángel and Unciti-Broceta, Asier and Díaz Mochón, Juan José},
}