Synthesis and Evaluation of Antifungal and Antitrypanosomastid Activities of Symmetrical 1,4-Disubstituted-1,2,3-Bistriazoles Obtained by CuAAC Conditions.

Synthesis and Evaluation of Antifungal and Antitrypanosomastid Activities of Symmetrical 1,4-Disubstituted-1,2,3-Bistriazoles Obtained by CuAAC Conditions.
Med Chem. 2018 Oct 24;:
Authors: Victor MM, Farias RR, da Silva DL, do Carmo PHF, de Resende-Stoianoff MA, Viegas C, Espurie PF, Marquese MJ
Abstract
BACKGROUND: The trypanosomatids, such as the protozoan Leishmania spp., have a demand by ergosterol, which is not present in the membrane from mammal cells. The suppression of the synthesis of ergosterol would be a new target of compounds with leishmanicidal activity, and bistriazole has showed trypanocidal activity by this mechanism. The incidence of fungal infections has increased at an alarming rate over the last decades. This is related both to the growing population of immune-compromised individuals and to the emergence of strains that are resistant to available antifungals. Therefore, there is a challenge for the search of potential new antifungal agents.
OBJECTIVE: the study aimed to synthesized 1,4-disubstituted-1,2,3-bistriazoles by optimized copper(I)-catalyzed alkyne-azide cycloaddition (CuAAC) and evaluate their antifungal and antitrypanosomastid activities.
METHOD: The synthesis of symmetrical bistriazoles with diazides as spacers was planned to be performed following the CuAAC reaction strategy. For evaluation of best conditions to synthesis of symmetrical bistriazoles hex-1-yne 2 was choose as leading c...

Source: Medicinal Chemistry - October 24, 2018 Category: Chemistry Authors: Victor MM, Farias RR, da Silva DL, do Carmo PHF, de Resende-Stoianoff MA, Viegas C, Espurie PF, Marquese MJ Tags: Med Chem Source Type: research