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Sci. Pharm.
Volume 74
Issue 3
10.3797/scipharm.2006.74.85
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Article

Ureidopyridazine Derivatives as Acyl-CoA: cholesterol acyltransferase Inhibitors

by
Arianna Gelain
1,
Ilaria Bettinelli
1,
Daniela Barlocco
1,*,
Byoung-Mog Kwon
2,
Tae-Sook Jeong
2,
Kyung-Ran Im
2,
Laura Legnani
3 and
Lucio Toma
3,*
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.
Sci. Pharm. 2006, 74(3), 85-97; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.2006.74.85
Submission received: 29 August 2006 / Accepted: 6 September 2006 / Published: 30 September 2006
Versions Notes

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

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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. https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.2006.74.85

AMA 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. Scientia Pharmaceutica. 2006; 74(3):85-97. https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.2006.74.85

Chicago/Turabian Style

Gelain, Arianna, Ilaria Bettinelli, Daniela Barlocco, Byoung-Mog Kwon, Tae-Sook Jeong, Kyung-Ran Im, Laura Legnani, and Lucio Toma. 2006. "Ureidopyridazine Derivatives as Acyl-CoA: cholesterol acyltransferase Inhibitors" Scientia Pharmaceutica 74, no. 3: 85-97. https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.2006.74.85

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