Synthesis and anti-hyperlipidemic evaluation of N‑(benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide derivatives in Triton WR-1339-induced hyperlipidemic rats

Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
Ghassan ShattatMoyad Shahwan

Abstract

The lipid-lowering activity of a series of novel N-(benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide derivatives has been studied in Triton WR-1339-induced hyperlipidemia in rats. The test animals were divided into four groups: control, hyperlipidemic, compound + 4% DMSO [C1: N-(2-benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide (1), C2: N-(3-benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide (2), C3: N-(4-benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide (3)]-treated and bezafibrate (BF)-treated. At a dose of 15 mg/Kg body weight, compounds 2, 3 and BF significantly reduced elevated plasma triglycerodes levels after 12 h. Moreover, high density lipoprotein-cholesterol levels were significantly increased in all treated groups after 12 h compared to the hyperlipidemic control group, except for C1 which was inactive. In sum, it may be stated that the results of the present study demonstrated new properties of some N-(benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide derivatives as potent lipid lowering agents and these beneficial activities may contribute to their cardioprotective and antiatherosclerotic role.

References

Jan 1, 1987·International Journal of Immunopharmacology·L J RobichaudR L Adolphson
Jul 31, 1998·The American Journal of Medicine·W H Frishman
Nov 10, 1998·Circulation·B StaelsJ C Fruchart
Dec 18, 2001·Journal of Ethnopharmacology·L Anila, N R Vijayalakshmi
Jul 13, 2004·Bioorganic & Medicinal Chemistry·Guixia LiuHualiang Jiang
Dec 5, 2009·Zeitschrift Für Naturforschung. C, a Journal of Biosciences·Tariq Al-QirimSyed Zaidi

Citations

Jun 5, 2014·Bioorganic & Medicinal Chemistry·Nariman F Salakhutdinov, Sergey S Laev
Dec 29, 2015·Bioorganic & Medicinal Chemistry Letters·Santosh N MokalePankaj B Miniyar
Sep 12, 2015·European Journal of Medicinal Chemistry·Rémi CaraballoMikael Elofsson
Aug 26, 2016·Journal of Enzyme Inhibition and Medicinal Chemistry·Rana Abu FarhaRabab Albashiti
Sep 7, 2016·Drug Development and Industrial Pharmacy·Divya Suares, Bala Prabhakar
Apr 3, 2018·Chemical & Pharmaceutical Bulletin·Ghassan Abu SheikhaYusuf Al-Hiari
Sep 6, 2018·The Journal of Pharmacy and Pharmacology·Gaurav GargAmitava Chakrabarti

Methods Mentioned

BETA
column chromatography

Related Concepts

Translight
N-(benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide
Hypolipidemic Agents
Bezamerck
Lipidemias
Indoles
High Density Lipoprotein Cholesterol
Vigilon
Structure-Activity Relationship
Rats, Wistar

Related Feeds

ApoE, Lipids & Cholesterol

Serum cholesterol, triglycerides, apolipoprotein B (APOB)-containing lipoproteins (very low-density lipoprotein (VLDL), immediate-density lipoprotein (IDL), and low-density lipoprotein (LDL), lipoprotein A (LPA)) and the total cholesterol/high-density lipoprotein (HDL) cholesterol ratio are all connected in diseases. Here is the latest research.