3-heptylamino-5-phenylpyridazine derivatives as analogues of Acyl-CoA: cholesterol acyltransferase inhibitors containing the N-heptyl-N'-arylureidic moiety = 페닐피리다진 유도체의 ACAT 저해활성

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Title
3-heptylamino-5-phenylpyridazine derivatives as analogues of Acyl-CoA: cholesterol acyltransferase inhibitors containing the N-heptyl-N'-arylureidic moiety = 페닐피리다진 유도체의 ACAT 저해활성
Author(s)
A Gelain; D Barlocco; Byoung-Mog Kwon; Tae Sook Jeong; Kyung-Ran Im; L Legnani; L Toma
Bibliographic Citation
Archiv der Pharmazie, vol. 339, no. 12, pp. 645-651
Publication Year
2006
Abstract
A series of novel Acyl-CoA: cholesterol acyltransferase (ACAT) inhibitors 8a-f was synthesized; the substances were characterized by the presence of a 2,5-dimethylpyrazin-3-yl moiety at one end and a 3-heptylamino-5- phenylpyridazine system at the other one, linked through linear alkyl spacers of different length. The new derivatives were designed based on the hypothesis that the 3-amino-5-phenylpyridazine moiety could mimic the aryl substituted urea, which was present in a number of ACAT inhibitors previously described. The choice of the 2,5-dimethylpyrazin-3-yl substituent was supported by a preliminary investigation, which indicated that this moiety is the most powerful in conferring ACAT inhibitory properties to the new series. The pharmacological results proved the idea to be sound. Finally, compounds 9a-c, lacking the phenylpyridazine moiety were prepared and tested to further strengthen our hypothesis.
Keyword
ACAT inhibitorshypercholesterolemiapyridazine derivativesureido analogues
ISSN
0365-6233
Publisher
Wiley
DOI
http://dx.doi.org/10.1002/ardp.200600106
Type
Article
Appears in Collections:
Division of Biomedical Research > Microbiome Convergence Research Center > 1. Journal Articles
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