A series of novel lipophilic polyamines was synthesized by the sodium cyanoborohydride-mediated reductive amination of various ketones and aldehydes with the polyamine tris(2-aminoethyl)amine. Two of these compounds, N,N-bis[2-(cyclododecylamino)ethyl]-N'-benzyl-1,2-ethanediamine trihydrochloride (36.3HCl) and N,N-bis[2-(cyclododecylmethylamino)ethyl]-N',N'-dimethyl-1,2-ethan ediamine (23), are 29 and 24 times more potent than colestipol hydrochloride, respectively, for lowering animal serum cholesterol levels.

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm00085a011DOI Listing

Publication Analysis

Top Keywords

novel lipophilic
8
lipophilic polyamines
8
cholesterol lowering
4
lowering bile
4
bile acid
4
acid binding
4
binding agents
4
agents novel
4
polyamines series
4
series novel
4

Similar Publications

Herein we report the synthesis of a novel di-O-acylated DNJ derivative, conceived to study whether iminosugar derivatization with a lipophilic acyl moiety could positively affect its antibacterial properties. The well-known PS-TPP/I/ImH activating system was used to readily install the acyl chains on the iminosugar, leading to the desired compound in high yield. Biological assays revealed that a di-O-lauroyl DNJ derivative enhanced the antibacterial effect of gentamicin and amikacin against S.

View Article and Find Full Text PDF

Phthalates are the emerging environmental toxicants derived from phthalic acid and its constituents, which are moderately present in plastics and many personal care products. Phthalate exposure occurs through various environmental factors, including air, water, and soil, with absorption facilitated via ingestion, inhalation, and dermal contact. Upon exposure, phthalates become bioavailable within the biological systems and undergo biotransformation and detoxification processes in the liver.

View Article and Find Full Text PDF

Alzheimer's disease (AD) is the most common form of dementia, marked by progressive brain degeneration and cognitive decline. A major pathological feature of AD is the accumulation of hyperphosphorylated tau (p-tau) in the form of neurofibrillary tangles (NFTs), which leads to neuronal death and neurodegeneration. P-tau also induces endoplasmic reticulum (ER) stress and activates the unfolded protein response, causing inflammation and apoptosis.

View Article and Find Full Text PDF

Novel ionic liquid catalysts comprising terephthalate anions are capable of promoting the neutral hydrolysis of relatively large flake sizes of poly(ethylene terephthalate) at 0.5 mol% loading (200 °C, 4 h, 94% yield) without either attendant product inhibition or product contamination by protonated catalyst. Catalysts with large, lipophilic phosphonium cations outperform more polar variants.

View Article and Find Full Text PDF

A peptide segment that is 10 residues long at the C-terminal (CT) region of Cx43 is known to be involved in interactions, both with the Cx43 protein itself and with other proteins, that result in hemichannel (HC) activity regulation. Previously reported mimetic peptides based on this region (, , ) have been revealed to be promising therapeutic agents in the context of cardiovascular diseases. In this work, novel approaches, such as C- and N-terminal modification and cyclization, to improve the proteolytic stability and bioavailability of the peptide are presented.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!