Next Article in Journal
Synthesis and Pharmacological Evaluation of New 2-Substituted-5-{2-[(2-halobenzyl)thio)phenyl}-1,3,4-oxadiazoles as Anticonvulsant Agents
Previous Article in Journal
Tirofiban Preserves Endothelial Junctions and Decreases Endothelin-1
Article Menu

Article Versions

Export Article

Scientia Pharmaceutica is published by MDPI from Volume 84 Issue 3 (2015). Articles in this Issue were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) licence. Articles are hosted by MDPI on mdpi.com as a courtesy and upon agreement with Austrian Pharmaceutical Society (Österreichische Pharmazeutische Gesellschaft, ÖPhG).
Open AccessArticle
Sci. Pharm. 2006, 74(3), 85-97; https://doi.org/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
PDF [331 KB, uploaded 27 December 2016]

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).

Share & Cite This Article

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.

Show more citation formats Show less citations formats

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Sci. Pharm. EISSN 2218-0532 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top