ChemInform Abstract: Solution‐Phase Parallel Synthesis of Novel 1,2,3,4‐Tetrahydroisoquinolin‐1‐ones as Anticonvulsant Agents.

Abstract

2,3,4-Tetrahydroisoquinolin-1-ones as Anticonvulsant Agents. -A series of 13 PD00735 analogues of type (IV)/(V) is prepared and their anticonvulsant activities are studied. All of the compounds are less active than PD00735 with (IVb) and (IVc) showing the highest activities. -(GITTO*, R.; FRANCICA, E.; DE SARRO, G.; SCICCHITANO, F.; CHIMIRRI, A.; Chem.

Methyltrans-(±)-1-oxo-2-phenethyl-3-(thiophen-2-yl)-1,2,3,4-tetrahydroisoquinoline-4-carboxylate

“…Compounds containing tetrahydroisoquinoline fragment in their structure display a broad spectrum of biological activities. In particular, derivatives of this type have been recently recognized as being G-protein-coupled receptor 40 (GPR40) antagonists (Humphries et al2009), inhibitors of the MDM2-p53 interaction (Rothweiler et al, 2008), potent anticonvulsant agents (Gitto et al, 2008), etc. Thus, the title compound (I) was synthesized as a part of our ongoing program related to anhydride-based synthesis of new heterocyclic compounds with potential pharmacological activities (Bogdanov et al, 2007;Burdzhiev & Stanoeva, 2006;Kandinska et al, 2006).…”