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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

Authors 

A GelainD BarloccoByoung-Mog KwonTae Sook JeongKyung-Ran ImL LegnaniL Toma

Publisher 

Wiley-Blackwell

Issue Date 

2006

Citation 

Archiv der Pharmazie, vol. 339, no. 12, pp. 645-651

Keywords 

ACAT inhibitorshypercholesterolemiapyridazine derivativesureido analogues3 heptylamino 5 phenylpyridazine derivativecholesterol acyltransferase inhibitorpolycyclic aromatic hydrocarbon derivativepyridazine derivativeenzyme inhibitorssterol o-acyltransferase

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.

ISSN 

0365-6233

Link 

http://dx.doi.org/10.1002/ardp.200600106

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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