Pharmacological Evaluation of Novel Indole-2-carboxamides As Potent Lipid-Lowering Agents in Triton-WR-1339-Induced Hyperlipidemic Rats

Abstract

The lipid-lowering effects of two novel antihyperlipidemic agents, BMI2C [N-(4-benzoylphenyl)-5-methoxy-1H-indole-2-carboxamide] and DDMI2C [N-(9,10-dihydro-9,10-dioxoanthracen-2-yl)-5-methoxy-1H-indole-2-carboxamide], were studied using hyperlipidemic rats as an experimental model; hyperlipidemia was developed by intraperitoneal injection of Triton WR-1339 (200 mg/kg body weight). At a dose of 15 mg/kg body weight, BMI2C and DDMI2C signifi cantly reduced elevated plasma triglyceride levels after 7 and 24 h. Furthermore, BMI2C and DDMI2C signifi cantly reduced elevated plasma total cholesterol levels after 24 h. Interestingly, high-density lipoprotein-cholesterol levels were signifi cantly increased in all treated groups. These fi ndings indicate that the two studied novel compounds have a promising potential in the treatment of hyperlipidemia and atherosclerosis. Key words: BMI2C [N-(4-Benzoylphenyl)-5-methoxy-1H-indole-2-carboxamide], DDMI2C[N-(9,10-Dihydro-9,10-dioxoanthracen-2-yl)-5-methoxy-1H-indole-2-carboxa mide], Antihyperlipidemic Activity

Synthesis and <i>in vivo</i> anti-hyperlipidemic activity of novel n-benzoylphenyl-2-furamide derivatives in Wistar rats

“…The findings of this research work are in agreement with our previous data which indicated that the presence of an aromatic heterocyclic moiety connected to huge lipophilic aromatic rings through a carboxamide linkage is necessary for interaction with proper target(s) for hypolipidemic activity [25,26]. Also, the chemical nature and the electronic effect of the substituents bearing on the heterocycle ring play an important role in the determination of activity.…”

Antihyperlipidemic Properties of Novel N-(Benzoylphenyl)-5-substituted-1H-indole-2-carboxamides in Triton WR-1339-Induced Hyperlipidemic Rats

“…During the last decade, a lot of attention has been given to studies focused on the synthesis of indole containing agents and their pharmacological activities. From these studies, which include our previously published work, it was found that compounds containing the indole-2-carboxamodes have a promising potential effects as lipid-lowering agents [ 14 , 15 , 16 , 17 , 18 , 19 , 20 ]. Previous work by our group revealed that N-(benzoylphenyl)-5-fluoro-1 H -indole-2-carboxamide derivatives ( Figure 1 ) exhibited significant hypolipidemic effects [ 19 ].…”

Synthesis and Anti-Hyperlipidemic Evaluation of N‑(Benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide Derivatives in Triton WR-1339-Induced Hyperlipidemic Rats

“…Some indole derivatives are well-known for their diverse pharmacological effects including a hypolipidemic effect [ 11 , 12 , 13 , 14 , 15 ]. Although studies have shown the potential role for indole-2-carboxamide derivatives as anti-allergics [ 16 ], and antioxidants [ 17 , 18 ],to the best of our knowledge N -(benzoylphenyl)-5-fluoro-1 H -indole-2-carboxamide derivatives have not been investigated as potential lipid-lowering agents.…”