392231-82-2Relevant academic research and scientific papers
Synthesis and biological evaluation of 4,5,6,7-tetrahydrothieno[2,3-c]pyridine–based β-aminonitriles and their derivatives: β-amino carboxamides, (thio)ureas, and tetracycles
Hackler, László,Kanizsai, Iván,Kari, Beáta,Madácsi, Ramóna,Nagy, Lajos I.,Puskás, László G.,Traj, Péter
, (2019)
The preparation and cytotoxic characterization of 4,5,6,7-tetrahydrothieno[2,3-c]pyridine–based β-aminonitriles, β-amino carboxamides, and their (thio)urea and annulated derivatives were accomplished. Following a synthetic route involving Gewald three-component reactions (G-3CR) and a Lewis acid–catalyzed iso (thio)cyanate coupling, 30 compounds were prepared for antitumor evaluation. For derivatizations, a catalytic amount of CuOAc2 (20 mol%) was essential for improving the reactivity of either the C-2 amino function of thiophene or isocyanates. The synthesized analogues demonstrated a weak to moderate antitumor activity in a low micromolar range against A549 and K562 cancer cell lines.
Cyclic amine sulfonamides as linkers in the design and synthesis of novel human β3 adrenergic receptor agonists
Sum, Fuk-Wah,Wong, Victoria,Han, Stella,Largis, Elwood,Mulvey, Ruth,Tillett, Jeff
, p. 2191 - 2194 (2007/10/03)
Piperidine, pyrrolidine, and azetidine sulfonamides were examined as linkers in designing novel human β3 adrenergic receptor (β3-AR) agonists. The azetidine derivative 37, and piperidine derivatives 7, 8, and 13 were found to be potent β3-AR agonists and have good selectivity against β1- and β2-AR.
