Журнал гликомики и липидомики
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Synthesis and hypolipidemic properties of novel N-(4-benzoylphenyl) pyrrole-2-carboxamide derivatives

Tariq Al-Qirim

Hyperlipidemia is involved in development of atherosclerosis and coronary heart disease. We synthesized two novel pyrrole carboxamide derivatives N-(4-benzoylphenyl)-4-bromo-2,5-dihydro-1H-pyrrole-2 carboxamide (1) and 4- Amino-N-(4- benzoylphenyl)-1-methyl-1H- pyrrole-2carboxamide (2) and tested them as anti-hyperlipidemic agents. The synthesized compounds were characterized using IR and NMR. Biological evaluation of compound 1 and 2 showed that compound 1 significantly decreased TG, LDL-C and TC, and mild increase in HDL-C in plasma. Contrarily, compound 2 appeared to be less potent when compared to 1; it moderately decreased TG, LDL-C and TC with mild increase of HDL-C. The NH pyrrole mediates H-bond interaction of 1 with the backbone of the target(s) protein(s) and this corresponds to the high potency of 1. The lower activity of 2 confirms that the presence of H-bond is essential to induce high activity. The finding of this work suggests that this scaffold might be promising as antihyperlipidemic agents for future work.