26646-43-5Relevant academic research and scientific papers
Towards new 5-HT7 antagonists among arylsulfonamide derivatives of (aryloxy)ethyl-alkyl amines: Multiobjective based design, synthesis, and antidepressant and anxiolytic properties
Canale, Vittorio,Kurczab, Rafa,Partyka, Anna,Sataa, Grzegorz,Ledna, Tomasz,Jastrzebska-Wiesek, Magdalena,Wesoowska, Anna,Bojarski, Andrzej J.,Zajdel, Pawel
, p. 334 - 346 (2016)
A series of 39 arylsulfonamide/amide derivatives of (aryloxy)ethyl alkyl amines, was designed with the support of the Virtual Combinatorial Library-Virtual Screening protocol, and synthesized using solidphase methodologies. Representative compounds were biologically evaluated for their affinity for 5-HT7Rs and for their selectivity over related 5-HTRs (5-HT1ARs, 5-HT2ARs, 5-HT6Rs), dopamine D2Rs and adrenergic a1Rs. The study identified the derivatives 27 (3-fluoro-N-{1-[2-(2-cyclopentylphenoxy) ethyl]piperidin-4-yl}-benzenesulfonamide; PZ-1417) and 35 (4-fluoro-N-(1-{2-[(propan-2-yl)phenoxy] ethyl}-8-azabicyclo[3.2.1]octan-3-yl)-benzenesulfonamide; PZ-1150) as being potent 5-HT7R antagonists with antidepressant and anxiolytic properties in the forced swim test (0.625e5 mg/kg and 0.625 mg/kg, respectively), the tail suspension test (0.625 mg/kg and 0.625 mg/kg, respectively), and in four plate test (0.625 mg/kg and 1.25e2.5 mg/kg, respectively) in mice. It has to be stressed that new compounds displayed higher activity than that of SB-269970, a reference 5-HT7R antagonist. Finally, the study provided valuable insight into the development of potential therapeutic agents for the treatment of CNS disorders.
A simple modification of the known preparation procedure of 2-Phenoxyethyl bromides providing high yields
Slyn'ko,Tormyshev
, p. 254 - 257 (2007/10/03)
A modification of preparation method was developed for synthesis of a number of 1-bromo-2-phenoxyethanes from 1,2-dibromoethanes and sodium phenolates in two-phase water-organic system with or without addition of triethylbenzylammonium chloride as phase-transfer catalyst. Addition of NaOH in two portions for transforming phenols into phenolates ensured high yields (60-80%) of phenoxylation products.
