Antiarrhythmic, serotonin antagonist and antianxiety activities of novel substituted thiophene derivatives synthesized from 2-amino-4,5,6,7-tetrahydro-N-phenylbenzo[b]thiophene-3-carboxamide

作者：Amr Abd El Galil E^*; Sherif Mohamed H; Assy Mohamed G; Al Omar Mohamed A; Ragab Islam

来源：European Journal of Medicinal Chemistry, 2010, 45(12): 5935-5942.

DOI：10.1016/j.ejmech.2010.09.059

• Thiophenes
• Thiazoles
• Oxazinones
• Antiarrhythmic
• Serotonin antagonist and antianxiety activities

A series of novel thiophene derivatives 3-17 were synthesized by initial reactions of 2-amino-4,5,6,7-tetrahydro-N-phenylbenzo[b]thiophene-3-carboxamide I and 2-amino-4,5,6,7-tetrahydro-benzo[b] thiophene-3-carbonitrile 7 with different organic reagents. The structures of newly synthesized compounds were confirmed by IR, (1)H NMR, MS spectral data and elemental analysis. Initially the acute toxicity of the compounds was assayed via the determination of their LD(50). All the compounds were screened for their antiarrhythmic, serotonin antagonist and antianexiety activities and they showed high activity compared with procaine amide, lidocaine, diazepam and buspirone as positive controls. The detailed synthesis, spectroscopic data, LD(50) and pharmacological activities of the synthesized compounds were reported.

• 出版日期2010-12