Synthesis of trans- and cis-2-acetyl-3-phenyl-3,3a,4,5-tetrahydro-2H-benzo[g] indazoles: evaluation as inhibitors of β-hematin formation

Abstract:

Several trans- and cis-2-acetyl-3-(substituted-phenyl)-3,3a,4,5-tetrahydro-2H-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.

Año de publicación:

2017

Keywords:

• Indazoles
• Β-hematin
• Diastereomers
• Pyrazolines
• MALARIA
• Hydrazine

Fuente:

scopus