Esters of some non-steroidal anti-inflammatory drugs with cinnamyl alcohol are potent lipoxygenase inhibitors with enhanced anti-inflammatory activity.
Novel esters of non steroidal anti-inflammatory drugs, α-lipoic acid and indol-3-acetic acid with cinnamyl alcohol were synthesised by a straightforward method and at high yields (60-98%). They reduced acute inflammation more than the parent acids and are potent inhibitors of soybean lipoxygenase. Selected structures decreased plasma lipidemic indices in Triton-induced hyperlipidemia to rats. Therefore, the synthesised compounds may add to the current knowledge about agents acting against various inflammatory disorders.
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Thessaloniki 54124, Greece.
Panagiotis
P
Theodosis-Nobelos
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Thessaloniki 54124, Greece.
Malamati
M
Kourti
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Thessaloniki 54124, Greece.
Paraskevi
P
Tziona
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Thessaloniki 54124, Greece.
Panos N
PN
Kourounakis
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Thessaloniki 54124, Greece. Electronic address: rekka@pharm.auth.gr.
Eleni A
EA
Rekka
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D002351:Carrageenan; D002934:Cinnamates / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D004952:Esters; D006949:Hyperlipidemias / Q000139:chemically induced / Q000188:drug therapy; D007210:Indoleacetic Acids / Q000737:chemistry; D016859:Lipoxygenase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D011092:Polyethylene Glycols; D020005:Propanols / Q000737:chemistry*; D011422:Propionates / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D051381:Rats; D013025:Glycine max; D008063:Thioctic Acid / Q000737:chemistry
D000894:Anti-Inflammatory Agents, Non-Steroidal; D002934:Cinnamates; D004952:Esters; D007210:Indoleacetic Acids; D016859:Lipoxygenase Inhibitors; D020005:Propanols; D011422:Propionates; C000609659:cinnamyl 2-(4-isobutylphenyl)propanoate; D011092:Polyethylene Glycols; C030737:indoleacetic acid; D008063:Thioctic Acid; D002351:Carrageenan; C020722:cinnamyl alcohol; C016811:tyloxapol
Cinnamyl esters; Dyslipidemia; Inflammation; Lipoxygenase inhibition; Non steroidal anti-inflammatory drugs