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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