Multitarget AD inhibitor-1

Multitarget AD inhibitor-1 is a selective and reversible butyrylcholinesterase (BuChE) inhibitor with IC50s of 7.22 μM and 1.55 μM for hBuChE and eqBuChE, respectively. Multitarget AD inhibitor-1 inhibits β-secretase (IC50hBACE-1=41.60 μM), amyloid β aggregation (IC50 Aβ=3.09 μM), tau aggregation (55% at 10 μM). Multitarget AD inhibitor-1, a diphenylpropylamine derivative, has the potential for multifunctional disease-modifying anti-Alzheimer’s[1].

Signaling Pathways >> Neuronal Signaling >> Beta-secretase

Research Areas >> Neurological Disease

Multitarget AD inhibitor-1 (compound 10) selectively inhibits BuChE from equine serum (eqBuChE) and hBuChE over AChE from electric eel (eeAChE; 21.78% at 10 μM)[1]. Multitarget AD inhibitor-1 (10 μM) inhibits full-length tau aggregation with 44.4%[1].

[1]. Dawid Panek, et al. Design, Synthesis, and Biological Evaluation of 1-Benzylamino-2-hydroxyalkyl Derivatives as New Potential Disease-Modifying Multifunctional Anti-Alzheimer's Agents. ACS Chem Neurosci. 2018 May 16;9(5):1074-1094.