Ureidopyridazine Derivatives as Acyl-CoA: cholesterol acyltransferase Inhibitors

Gelain, Arianna; Bettinelli, Ilaria; Barlocco, Daniela; Kwon, Byoung-Mog; Jeong, Tae-Sook; Im, Kyung-Ran; Legnani, Laura; Toma, Lucio

doi:10.3797/scipharm.2006.74.85

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Article

30 September 2006

13 Pages

Ureidopyridazine Derivatives as Acyl-CoA: cholesterol acyltransferase Inhibitors

and

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

Korea Research Institute of Bioscience & Biotechnology, 52 Uen-Dong Yusung- Ku, Taejeon 305-600, Korea

Dipartimento di Chimica Organica, Università di Pavia, Via Taramelli 10, 27100 Pavia, Italy

Authors to whom correspondence should be addressed.

Sci. Pharm.2006, 74(3), 85-97;https://doi.org/10.3797/scipharm.2006.74.85

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Abstract

A series of N-(2,4-difluorophenyl)-N’-heptyl-N’-{4-[(substituted)-pyridazin-3-yl)thio]pentyl}urea derivatives having a phenyl ring at positions 5 and/or at position 6 of the heterocycle, as well as the corresponding sulfones, were synthesized. 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 their activity to their structural features.

Keywords:

Hypercholesterolemia; ACAT inhibitors; pyridazine derivatives; ureido derivatives

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