Synthesis of Trans- and cis -2-acetyl-3-phenyl-3,3a,4,5-tetrahydro-2 H -benzo[ g ] Indazoles: Evaluation as Inhibitors of β-hematin Formation

Several trans- and cis-2-acetyl-3-(substituted-phenyl)-3,3a,4,5-tetrahydro-2 H-benzo[ g]indazole derivatives have been synthesised via the condensation of the appropriate exocyclic α,β-unsaturated ketones with hydrazine in hot acetic acid, to obtain diastereomeric mixtures of N-acetylated isomers. S...

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Published inJournal of chemical research Vol. 41; no. 11; pp. 668 - 672
Main Authors Aparicio, Daniel A., Lobo, Gricela M., Sánchez, Jennifer L., Monasterios, Melina C., Acosta, María E., De Lima, Lola, Llovera, Ligia J., Ángel, Jorge E., Charris, Jaime E.
Format Journal Article
LanguageEnglish
Published 01.11.2017
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Summary:Several trans- and cis-2-acetyl-3-(substituted-phenyl)-3,3a,4,5-tetrahydro-2 H-benzo[ g]indazole derivatives have been synthesised via the condensation of the appropriate exocyclic α,β-unsaturated ketones with hydrazine in hot acetic acid, to obtain diastereomeric mixtures of N-acetylated isomers. Structure elucidation was based on their spectral data and the trans–cis stereochemistry using of NOE and NOESY experiments. Biological testing of these derivatives as inhibitors of β-hematin formation was carried out.
ISSN:1747-5198
2047-6507
DOI:10.3184/174751917X15105690662845