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Paper | Regular issue | Vol 53, No. 12, 2000, pp.2709-2718
Published online, 1st January, 1970
DOI: 10.3987/COM-00-9037
5,6-Dinitrophenyl and 5-Aminophenyl-6-nitrophenyl Analogues of the ACAT Inhibitor 5,6-Diphenyl-3-alkylaminopyridazines

Lucio Toma,* Donatella Nava, Giuseppe Celentano, Maria Paola Giovannoni, Vittorio Dal Piaz, Byoung-Mog Kwon, Mi-Kyiung Kim, Young-Kook Kim, and Daniela Barlocco*

*Istituto di Chimica Farmaceutica e Tossicologica, Università di Milano, Viale Abruzzi 42, 20131 Milano, Italy

Abstract

A series of dinitro and monoamino-mononitro analogues of the 5,6-diphenyl-3-alkylaminopyridazines were synthesized and their structure was assigned on the basis of mono and bidimensional NMR experiments. Their inhibitory activity against acyl-CoA:cholesterol acyltransferase (ACAT) was tested on the enzyme prepared from rat liver microsomes. Theoretical studies were performed to correlate the activity of the compounds to their structural features.