ChemInform Abstract: 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.

Abstract

Synthesized from 2-Amino-4,5,6,7-tetrahydro--N-phenylbenzo[b]thiophene-3-carboxamide. -The synthesis of a series of condensed thiophenes uses compounds (I) and (VI) as starting materials. All compounds show potent antiarrhythmic, antianxiety, and serotonin antagonist activities. The thiophene nucleus is essential for activity, and increasing the number of sulfur or nitrogen atoms sharply increases the activities. In addition, the olefinic bond in the substituted side chain leads to an increase of activity. -(AMR*, A. E.-G. E.; SHERIF, M. H.; ASSY, M. G.; AL-OMAR, M. A.; RAGAB, I.; Eur. J. Med. Chem. 45 (2010) 12, 5935-5942, http://dx.doi.org/10.

Synthesis and cytotoxicity of fused thiophene and pyrazole derivatives derived from 2-N-acetyl-3-cyano-4,5,6,7-tetrahydrobenzo[b]thiophene

“…Some similar compounds from benzothiophene series namely 3-(aryl)benzothieno[2,3-c]pyran-1-ones (tricyclic lactones) were prepared by a tandem one-pot Sonogashira coupling and intramolecular cyclization. Furthermore, the tetrahydrobenzo[b]thiophene nucleus was adopted as a scaffold for many antimicrobial (Refat and Fadda, 2013), antiviral (Dewal et al, 2012), antiarrhythmic, (Amr et al, 2010), and antitumor (Abbas et al, 2013) activities. A structure activity relationship was established for the heterocyclic compounds derived from benzo[b]thiophene series with antitumor properties were prepared (Ferreirra et al, 2009), as well as a series of N-(2-(5-fluoro-2-(4-fluorophenylthio)benzo [b]thiophen-3-yl)ethyl) acylamides, which were evaluated for their binding affinity and intrinsic activity at melatonin receptors (Mésangeau et al, 2011).…”