G. F. Makhaeva, I. V. Serkov, N. V. Kovaleva, E. V. Rudakova, N. P. Boltneva, E. A. Kochetkova, A. N. Proshin, S. O. Bachurin, “Novel conjugates of 4-amino-2,3-polymethylenequinolines and vanillin as potential multitarget agents for AD treatment”, Mendeleev Commun., 2021, Volume 31, Issue 5,Pages <nobr>606

This article is cited in 9 papers

Communications

Novel conjugates of 4-amino-2,3-polymethylenequinolines and vanillin as potential multitarget agents for AD treatment

G. F. Makhaeva^a, I. V. Serkov^a, N. V. Kovaleva^a, E. V. Rudakova^a, N. P. Boltneva^a, E. A. Kochetkova^b, A. N. Proshin^a, S. O. Bachurin^a

^a Institute of Physiologically Active Compounds, Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry, Russian Academy of Sciences, Chernogolovka, Moscow Region, Russian Federation
^b Institute of Mathematics, Information Technology and Science, Ivanovo State University, Ivanovo, Russian Federation

Abstract: A series of novel conjugates of 4-amino-2,3-polymethylene quinolines and phenolic antioxidant vanillin was synthesized by the condensation of aminoquinolines with vanillin followed by reduction of imines with sodium borohydride. The conjugates effectively inhibit AChE and BChE with preferable BChE inhibition and displace propidium from the PAS AChE. Compounds with aminoalkyl spacer have preferable esterase profile being more potent cholinesterases inhibitors with lower anti-CES activity and are the most potent antioxidants in ABTS and FRAP tests.

Language: English

DOI: 10.1016/j.mencom.2021.09.005

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