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

Ureidopyridazine Derivatives as Acyl-CoA: cholesterol acyltransferase Inhibitors

1
Istituto di Chimica Farmaceutica e Tossicologica, Università di Milano, Viale Abruzzi 42, 20131 Milano, Italy
2
Korea Research Institute of Bioscience & Biotechnology, 52 Uen-Dong Yusung- Ku, Taejeon 305-600, Korea
3
Dipartimento di Chimica Organica, Università di Pavia, Via Taramelli 10, 27100 Pavia, Italy
*
Authors to whom correspondence should be addressed.
Received: 29 August 2006 / Accepted: 6 September 2006 / Published: 30 September 2006
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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 Hypercholesterolemia; ACAT inhibitors; pyridazine derivatives; ureido derivatives
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Gelain, A.; Bettinelli, I.; Barlocco, D.; Kwon, B.-M.; Jeong, T.-S.; Im, K.-R.; Legnani, L.; Toma, L. Ureidopyridazine Derivatives as Acyl-CoA: cholesterol acyltransferase Inhibitors. Sci. Pharm. 2006, 74, 85-97.

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