Synthèses et activités psychotropes de 3,4-diarylpipéridines. Corrélation structure-activité et recherche d'une activité antihypertensive

In vitro evaluation and in silico screening of synthetic acetylcholinesterase inhibitors bearing functionalized piperidine pharmacophores

“…4 A large number of compounds bearing piperidine scaffold have entered into preclinical and clinical trials over the last few years. 5 In particular, 1,4-disubstituted piperidine scaffolds find useful applications as established drugs such as donepezil (Aricept ® , an acetylcholinesterase inhibitor in the treatment of Alzheimer's disease), naratriptan (Naramig ® , an agonist of 5-hydroxytryptamine (serotonin) receptor 1D and 5-hydroxytryptamine receptor 1B in the treatment of migraine headaches), risperidone (Risperdal ® ) and sertindole (Serdolect ® ) (both nonselective 5-hydroxytryptamine receptor 2A/dopamine D 2 receptor (5-HT/D 2 ) antagonists, currently in the treatment of schizophrenia), 6,7 and exhibit anti-hypertensive, 8 antibacterial, 9 antimalarial, 10 anticonvulsant, and anti-inflammatory activities. 11 Moreover, some of them have been found to possess enzyme inhibitory activity against farnesyl transferase (FTase is believed to play an important role in development of progeria and various forms of cancers) 10 or dihydroorotate dehydrogenase (DHODH) 5 and also found to be useful in Parkinson's disease involving the MAO-based mechanism.…”

One-pot multicomponent synthesis of highly substituted piperidines using p-toluenesulfonic acid monohydrate as catalyst

“…Polyfunctionalized heterocyclic compounds play important roles in the drug discovery process and analysis of drugs in late development. Piperidines and their analogues have received attention owing to their biological activities [8,9], e.g., they act as antimalarial [10], antihypertensive [11], antibacterial [12], anticonvulsant, and anti-inflammatory agents [13]. As a result, various synthetic approaches have been developed for the synthesis of piperidines based on intramolecular Mannich reaction onto iminium ions [14], imino DielsAlder reaction [15,16], aza-Prins cyclizations [17,18], intramolecular Michael reaction [19], and cyclopropane ring-opening/Conia-ene cyclization [20].…”

Design, preparation and characterization of a new ionic liquid, 1,3-disulfonic acid benzimidazolium chloride, as an efficient and recyclable catalyst for the synthesis of tetrahydropyridine under solvent-free conditions

“…6 Tetrahydropyridine derivatives are among the most important classes of nitrogen-containing heterocycles, they are found in many natural products, pharmaceutical agents, and functionalized 50 materials. 9-11 Tetrahydropyridines and compounds based on these core templates exhibit a wide range of biological activities such as anti-hypertensive, 12 neurotoxic activity, 13 anti-bacterial, 14 anticonvulsant, anti-inflammatory activities, 15 and antimalarial. 16 Although numerous methodologies have been for the synthesis of 55 functionalized tetrahydropyridines by using LaCl 3 .7H 2 O, 17 Lproline/TFA , 16 …”