Synthesis and Antimalarial Activities of a Diverse Set of Triazole??Containing Furamidine Analogues

…, SA Ward, GA Biagini, PG Bray, PM O'Neill

Index: Berger, Olivier; Kaniti, Archana; van Ba, Christophe Tran; Vial, Henri; Ward, Stephen A.; Biagini, Giancarlo A.; Bray, Patrick G.; O'Neill, Paul M. ChemMedChem, 2011 , vol. 6, # 11 p. 2094 - 2108

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Citation Number: 16

Abstract

Abstract Four different series of triazole diamidines have been prepared by the Pinner method from the corresponding triazole dinitriles. Copper-catalyzed “click chemistry” was used for the synthesis of 1, 4-and 4, 5-substituted triazoles, aryl magnesium acetylide reagents for the 1, 5-substituted triazoles, with a thermal dipolar addition reaction employed for the 2, 4-substituted triazoles. In vitro antimalarial activity against two different PfCRT- ...