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2020 3
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The Chemotype of Chromanones as a Privileged Scaffold for Multineurotarget Anti-Alzheimer Agents.
Keuler T, Lemke C, Elsinghorst PW, Iriepa I, Chioua M, Martínez-Grau MA, Beadle CD, Vetman T, López-Muñoz F, Wille T, Bartz U, Deuther-Conrad W, Marco-Contelles J, Gütschow M. Keuler T, et al. ACS Pharmacol Transl Sci. 2022 Oct 12;5(11):1097-1108. doi: 10.1021/acsptsci.2c00097. eCollection 2022 Nov 11. ACS Pharmacol Transl Sci. 2022. PMID: 36407962 Free PMC article.
Acetylcholinesterase Inhibition of Diversely Functionalized Quinolinones for Alzheimer's Disease Therapy.
Bautista-Aguilera ÓM, Ismaili L, Chioua M, Andrys R, Schmidt M, Bzonek P, Martínez-Grau MÁ, Beadle CD, Vetman T, López-Muñoz F, Iriepa I, Refouvelet B, Musilek K, Marco-Contelles J. Bautista-Aguilera ÓM, et al. Int J Mol Sci. 2020 May 30;21(11):3913. doi: 10.3390/ijms21113913. Int J Mol Sci. 2020. PMID: 32486316 Free PMC article.
In particular, molecule QN8 was found to be a potent and quite selective non-competitive inhibitor of hrAChE (IC(50) = 0.29 M), with K(i) value in nanomolar range (79 nM). Pertinent docking analysis confirmed this result, suggesting that this ligand is an interesting hit f …
In particular, molecule QN8 was found to be a potent and quite selective non-competitive inhibitor of hrAChE (IC(50) = 0.29 M), with …
Isoxazolotacrines as non-toxic and selective butyrylcholinesterase inhibitors for Alzheimer's disease.
Cherif O, Allouche F, Chabchoub F, Chioua M, Soriano E, Yañez M, Cacabelos R, Romero A, López MG, Marco-Contelles J. Cherif O, et al. Future Med Chem. 2014;6(17):1883-91. doi: 10.4155/fmc.14.115. Future Med Chem. 2014. PMID: 25495982
Novel 3-phenyl-5,6,7,8-tetrahydroisoxazolo[5,4-b]quinolin-4-amine (OC41) is a promising, 31% less toxic than tacrine in HepG2 cells, and selective reversible human butyrylcholinesterase inhibitor (IC50 = 5.08 1.12 M), also showing good drug-like properties according to the …
Novel 3-phenyl-5,6,7,8-tetrahydroisoxazolo[5,4-b]quinolin-4-amine (OC41) is a promising, 31% less toxic than tacrine in HepG2 cells, and sel …
Synthesis, antioxidant properties and neuroprotection of α-phenyl-tert-butylnitrone derived HomoBisNitrones in in vitro and in vivo ischemia models.
Chamorro B, Diez-Iriepa D, Merás-Sáiz B, Chioua M, García-Vieira D, Iriepa I, Hadjipavlou-Litina D, López-Muñoz F, Martínez-Murillo R, Gonzàlez-Nieto D, Fernández I, Marco-Contelles J, Oset-Gasque MJ. Chamorro B, et al. Sci Rep. 2020 Aug 25;10(1):14150. doi: 10.1038/s41598-020-70690-y. Sci Rep. 2020. PMID: 32843666 Free PMC article.