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Synthesis of indazol-4,7-dione derivatives as potential trypanocidal agents

✍ Scribed by Ricardo A. Tapia; Claudia Carrasco; Scarlet Ojeda; Cristian Salas; Jaime A. Valderrama; Antonio Morello; Yolanda Repetto


Publisher
Journal of Heterocyclic Chemistry
Year
2002
Tongue
English
Weight
45 KB
Volume
39
Category
Article
ISSN
0022-152X

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✦ Synopsis


Abstract

The synthesis of new indazol‐4,7‐dione derivatives via 1,3‐dipolar cycloaddition of diazomethane with 2,3‐dimethyl‐1,4‐benzoquinone (2) and 1,4‐naphthoquinone (7) followed by N‐alkylation of the pyrazol nitrogen atom of the corresponding quinones (3) and (8) with methyl chloroacetate is described. A series of amides from esters (5) and (10) were also obtained. These compounds were tested in vitro as potential anti‐trypanosomal agents. Compounds (4) and (8) were found to have significant activity.


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