Search Results (3)

Alzheimer’s Disease (AD) is a common neurodegenerative disorder characterized by memory loss and cognitive impairment. Its pathology has not been fully clarified and therefore highly effective treatments have not been obtained yet. Almost all the current treatment options aim to alleviate only the symptoms and not to eliminate the disease itself. Acetylcholinesterase inhibitors are the main therapeutic agents against AD, whereas oxidative stress and inflammation have been found to be of great significance for the development and progression of neurodegeneration. In this work, ethyl nipecotate (ethyl-piperidine-3-carboxylate), a heterocyclic carboxylic acid derivative, which acts as a GABA reuptake inhibitor and has been used in research for diseases involving GABAergic neurotransmission dysfunction, was amidated with various carboxylic acids bearing antioxidant and/or anti-inflammatory properties (e.g., ferulic acid, sinapic acid, butylated hydroxycinnamic acid). Most of our compounds have significant antioxidant potency as lipid peroxidation inhibitors (IC₅₀ as low as 20 μΜ), as oxidative protein glycation inhibitors (inhibition up to 57%), and act as DPPH reducing agents. Moreover, our compounds are moderate LOX inhibitors (up to 33% at 100 μΜ) and could reduce rat paw edema induced by carrageenan by up to 61%. Finally, some of them possessed inhibitory activity against acetylcholinesterase (IC₅₀ as low as to 47 μΜ). Our results indicate that our compounds could have the potentiality for further optimization as multi-targeting agents directed against AD. Full article

A novel route for the synthesis of new spirocyclic derivative is developed. The present work involves the synthesis of title compound 3 by Suzuki coupling of 3,5-difluorophenyl boronic acid with tert-butyl 1-(5-bromofuran-2-yl)-4-oxo-2,3,7-triazaspiro[4.5]dec-1-ene-7-carboxylate (2), which in turn prepared from the ethyl nipecotate (1). Newly prepared spirocyclic derivative (3) is characterized by IR, NMR and mass spectral data. Full article

A simple and novel route for synthesis of new spirocyclic compound is developed. The present work involves condensation of ethyl nipecotate with 2-furaldehyde followed by the MnO₂ oxidation to give the β-keto ester which upon reaction with hydrazine hydrate gives the spiro pyrazolone. Full article