Synthesis and biological evaluation of new 4H-pyrano[2,3-b]quinoline derivatives that block acetylcholinesterase and cell calcium signals, and cause neuroprotection against calcium overload and free radicals.
The synthesis and biological evaluation of ethyl 5-amino-4-(3-pyridyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrano[2,3-b]quinoline-3-carboxylates (9-11) is described. We have found that these compounds inhibit AChE with a mild potency, mitigates the [Ca(2+)](c) triggered by high K(+), and cause neuroprotection against Ca(2+) overloading and free radical-induced neuronal death.
Marco-Contelles
José
J
Laboratorio de Radicales Libres (IQOG, CSIC), C/Juan de la Cierva 3, 28006 Madrid, Spain. iqoc21@iqog.csic.es
León
Rafael
R
López
Manuela G
MG
García
Antonio G
AG
Villarroya
Mercedes
M
D000313:Adrenal Medulla / Q000187:drug effects; D000818:Animals; D002118:Calcium / Q000378:metabolism*; D020013:Calcium Signaling / Q000187:drug effects*; D002417:Cattle; D002460:Cell Line; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D019439:Chromaffin Cells / Q000187:drug effects; D004353:Drug Evaluation, Preclinical; D005609:Free Radicals; D007770:L-Lactate Dehydrogenase / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D018696:Neuroprotective Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D011714:Pyrans / Q000138:chemical synthesis* / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology
C517922:4H-pyrano(2,3-b)quinoline; D002800:Cholinesterase Inhibitors; D005609:Free Radicals; D018696:Neuroprotective Agents; D011714:Pyrans; D011804:Quinolines; D007770:L-Lactate Dehydrogenase; D002118:Calcium