Identification of β‐aminopyrrolidine containing peptides as β‐amyloid aggregation inhibitors for Alzheimer's disease

Abstract

Alzheimer's disease (AD) is caused by a series of events initiated by the production and aggregation of the amyloid β‐protein (Aβ). In the early stages of the disease, Aβ is released in a soluble form then progressively forms oligomeric, multimeric, and fibrillar aggregates, triggering neurodegeneration. Thus, development of inhibitors that initiate reverse Aβ aggregation is thought to be a logical approach in treating AD. In this context, we developed β‐aminopyrrolidine containing 12 mer peptide 3 which is very potent in inhibiting the Aβ aggregation and also reducing Aβ(42)‐induced cytotoxicity.

Inhibition of Human Cholinesterases and in vitro β‐Amyloid Aggregation by Rationally Designed Peptides

“…Similarly, Preetham et al. developed a β‐aminopyrrolidine containing 12‐mer peptides derived from the Aβ sequence displaying a potent antiaggregant activity [39] . No reports of peptides selectively inhibiting AChE‐induced Aβ aggregation were found in the literature.…”

“…sequence displaying a potent antiaggregant activity. [39] No reports of peptides selectively inhibiting AChE-induced Aβ aggregation were found in the literature.…”

Frustrated Lewis pairs in two-dimensional borocarbonitride for the facile synthesis of 3-aminoimidazo[1,2-α]pyridines using TMSCN as an isonitrile substitute

“…The synthesis of imidazo[1,2-a]pyridines from alcohols using a DMSO-propylphosphonic anhydride (T3P s ) medium as an oxidizing and cyclodehydrating agent has been reported, 22 but the main drawback of this protocol is the high cost of T3P s and the use of isocyanides. 23,24 Among metal-free catalysts, [25][26][27][28][29] boron (B)-based nonmetallic catalysts have attracted much attention in present research for various applications. [30][31][32][33][34][35][36] However, as an electron-deficient Lewis acid catalyst, the empty sp 2 orbital of boron can interact with the lone pair of electrons of nitrogen, which suppresses the catalytic activity of BCN.…”

“…23,24 Among metal-free catalysts, [25][26][27][28][29] boron (B)-based nonmetallic catalysts have attracted much attention in present research for various applications. [30][31][32][33][34][35][36] However, as an electron-deficient Lewis acid catalyst, the empty sp 2 orbital of boron can interact with the lone pair of electrons of nitrogen, which suppresses the catalytic activity of BCN. 37,38 Thus, to address the issue, we tried to explore the synergistic effect of the dual-site catalytic behavior of boron carbon nitride with unsaturated B and N atoms as an FLP for cyclization reactions.…”