Details

Autor(en) / Beteiligte

• Chan, Wai N.
• Hadley, Michael S
• Harling, John D.
• Herdon, Hugh J.
• Jerman, Jeffrey C.
• Orlek, Barry S.
• Stean, Tania O.
• Thompson, Mervyn
• Upton, Neil
• Ward, Robert W.

Titel

Identification of a series of 1,2,3,4-tetrahydroisoquinolinyl- benzamides with potential anticonvulsant activity

Ist Teil von

• Bioorganic & medicinal chemistry letters, 1998-10, Vol.8 (20), p.2903-2906

Ort / Verlag

Oxford: Elsevier Ltd

Erscheinungsjahr

1998

Quelle

Elsevier Journal Backfiles on ScienceDirect (DFG Nationallizenzen)

Beschreibungen/Notizen

• A series of N-(tetrahydroisoquinolinyl)-2-methoxybenzamides was identified by high-throughput screening at the novel SB-204269 binding site. SAR studies have provided compounds 4 and 14 with high affinity and good anticonvulsant activity in animal models. High-throughput screening with the selective ligand [ 3H] SB-204269 has revealed a series of tetrahydroisquinolinyl benzamides 2–18. Preliminary SAR analysis has led to the 5-isomer 4 (R=2-OMe, 4-Bu t) which showed high affinity and a good anticonvulsant profile in vivo.