Development of novel N-(6-methanesulfonyl-benzothiazol-2-yl)-3-(4-substituted-piperazin-1-yl)-propionamides with cholinesterase inhibition, anti-β-amyloid aggregation, neuroprotection and cognition enhancing properties for the therapy of Alzheimer's disease

Abstract

A novel series of benzothiazole–piperazine hybrids were rationally designed, synthesized, and evaluated as multifunctional ligands against Alzheimer's disease (AD).

Walnut-Derived Peptide Activates PINK1 via the NRF2/KEAP1/HO-1 Pathway, Promotes Mitophagy, and Alleviates Learning and Memory Impairments in a Mice Model

“…Cognitive impairment is often characterized by multifactorial features such as oxidative stress, mitochondrial dysfunction, and progressive neurons loss. 41 The mitochondrial respiratory chain is regarded as the main source of intracellular ROS, which are produced during oxidative metabolism. 42 The production of intracellular ROS correlates with mitochondrial dysfunction.…”

Pregnenolone derivatives for the treatment of Alzheimer's disease: synthesis, and in vitro inhibition of amyloid β1–42 peptide aggregation, acetylcholinesterase and carbonic anhydrase-II

“…The impact of synthesized compounds on self-mediated Ab aggregation was evaluated by using a thioavin T-based uorometric test. 10,[59][60][61] Initially pretreated Ab 1-42 peptide was dissolved in DMSO to prepare 100 mM stock solution. The Ab 1-42 peptide stock solution was diluted to a concentration of 10 mM in 150 mM phosphate buffer (pH 7.4) containing 150 mM NaCl prior to the incubations.…”

Identifying the Novel Inhibitors Against the Mycolic Acid Biosynthesis Pathway Target “mtFabH” of Mycobacterium tuberculosis

“…The structure-based virtual screening is one of the reliable strategies to identify a potential inhibitor in the drug development process (Meng et al, 2011). But the major challenge for existing docking tools is to deal with the flexibility of protein for which several efforts are ongoing (Forli et al, 2016;Sulimov et al, 2019;Mishra et al, 2020b). Thus, to understand the protein-ligand molecular interactions, MD simulation can provide an atomistic insight on the structural stability and dynamic of protein-ligand interactions (Prakash and Luthra, 2012;Panda et al, 2020).…”