NDLI: Synthesis, hypolipidemic, and anti-inflammatory activities of arylphthalimides

Content Provider	Springer Nature Link
Author	Assis, Shalom P. O. Araújo, Tiago Gomes Sena, Vera L. M. Catanho, Maria Teresa J. A. Ramos, Mozart N. Srivastava, Rajendra M. Lima, Vera L. M.
Copyright Year	2013
Abstract	Phthalimide and some N-substituted cyclic imides may be potent hypolipidemic agents, capable of reducing plasma cholesterol, and triglyceride levels. In this work, N-phenylphthalimide (5a), N-(2-nitrophenyl)phthalimide (5b), N-(3-nitrophenyl)phthalimide (5c), N-(4-nitrophenyl)phthalimide (5d), N-(4-bromophenyl)phthalimide (5e), N-(4-amidaphenyl)phthalimide (5f), N-(4-methylthiophenyl)phthalimide (5g), and N-(4-chlorophenyl)phthalimide (5h) were synthesized, and their effects on reducing lipid levels and as acute antiinflammatory agents in 3-month-old male Swiss mice were compared with phthalimide. To access their safety, the drugs were administered to determine the acute toxicity (LD50 value). In addition, the acute anti-inflammatory activity was evaluated via carrageenan-induced edema; and the effective dose was determined for compounds that showed the best anti-inflammatory activity in comparison with ibuprofen. The compound (5g) proved to be a more active hypolipidemic compound than phthalimide, at a dose level of 20 mg kg−1 day−1. The derivative (5g) reduced the plasmatic triglycerides and cholesterol levels by 54 and 41 %, respectively, while the percentages of reduction were 43 and 30 %, respectively, with phthalimide. The hypocholesterolemic and hypotriglyceridemic activities of the (5g) derivative were similar to that obtained with the commercially available drug, pravastatin. The anti-inflammatory activity of compound (5b) was similar to ibuprofen and aspirin at 250 mg kg−1. Taken together, it was demonstrated that the new phthalimide derivatives were able to increase HDL-cholesterol levels, along with reducing the cholesterol and triglyceride levels and carrageenan-induced edema in mice. Therefore, they may offer promise in the future as new hypolipidemic and anti-inflammatory agents.
Starting Page	708
Ending Page	716
Page Count	9
File Format	PDF
ISSN	10542523
Journal	Medicinal Chemistry Research
Volume Number	23
Issue Number	2
e-ISSN	15548120
Language	English
Publisher	Springer US
Publisher Date	2013-06-15
Publisher Place	New York
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Arylphthalimides Phthalimides Hypolipidemic activity Anti-inflammatory activity Hypolipidemia Pharmacology/Toxicology Biochemistry Cell Biology
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Pharmacology, Toxicology and Pharmaceutics

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