Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, El-Tahrir, St., Dokki, Riyadh 11451, Saudi Arabia.
Eur J Med Chem. 2010 Dec;45(12):5935-42. doi: 10.1016/j.ejmech.2010.09.059. Epub 2010 Oct 14.
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 1 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, 1H NMR, MS spectral data and elemental analysis. Initially the acute toxicity of the compounds was assayed via the determination of their LD50. 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, LD50 and pharmacological activities of the synthesized compounds were reported.
一系列新型噻吩衍生物 3-17 通过 2-氨基-4,5,6,7-四氢-N-苯基苯并[b]噻吩-3-甲酰胺 1 和 2-氨基-4,5,6,7-四氢苯并[b]噻吩-3-甲腈 7 与不同有机试剂的初始反应合成。新合成化合物的结构通过 IR、1H NMR、MS 谱数据和元素分析确认。最初通过测定 LD50 来测定化合物的急性毒性。所有化合物均进行了抗心律失常、5-羟色胺拮抗剂和抗焦虑活性筛选，与普鲁卡因酰胺、利多卡因、地西泮和丁螺环酮作为阳性对照相比，它们表现出高活性。报道了合成化合物的详细合成、光谱数据、LD50 和药理学活性。
