Bis-Amiridines as Acetylcholinesterase and Butyrylcholinesterase Inhibitors: N-Functionalization Determines the Multitarget Anti-Alzheimer's Activity Profile.
Makhaeva GF, Kovaleva NV, Boltneva NP, Rudakova EV, Lushchekina SV, Astakhova TY, Serkov IV, Proshin AN, Radchenko EV, Palyulin VA, Korabecny J, Soukup O, Bachurin SO, Richardson RJ.
Makhaeva GF, et al.
Molecules. 2022 Feb 4;27(3):1060. doi: 10.3390/molecules27031060.
Molecules. 2022.
PMID: 35164325
Free PMC article.
The lead compounds 3a-c exhibited an IC(50)(AChE) = 2.9-1.4 M, IC(50)(BChE) = 0.13-0.067 M, and 14-18% propidium displacement at 20 muM. Kinetic studies of compounds 3a and 5d indicated mixed-type reversible inhibition. Molecular docking revealed favorable poses in both ca …
The lead compounds 3a-c exhibited an IC(50)(AChE) = 2.9-1.4 M, IC(50)(BChE) = 0.13-0.067 M, and 14-18% propidium displacement at 20 muM. Kin …