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ChemInform Abstract: Synthesis and Biological Evaluation of New Cyclopenteno[b]thiophene Derivatives as Local Anesthetic and Antiarrhythmic Agents.

✍ Scribed by A. M. AL-OBAID; H. I. EL-SUBBAGH; O. A. AL-SHABANAH; M. A. MAHRAN

Publisher: John Wiley and Sons
Year: 2010
Weight: 34 KB
Volume: 29
Category: Article
ISSN: 0931-7597
DOI: 10.1002/chin.199818130

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✦ Synopsis

Synthesis and Biological Evaluation of New Cyclopenteno[b]thiophene Derivatives as Local Anesthetic and Antiarrhythmic Agents. -A series of new 2-aminocyclopentenothiophene-3-carboxylates such as (V) and (VI) (12 examples in all) are synthesized as carticaine analogues. Compounds (Va), (Vc), (Vd), (VIa), and (VIc) exhibit local anesthetic and antiarrhythmic activity comparable to carticaine and lidocaine. The antiarrhythmic potency proceeds via blocked Na + channels (e.g. (VIc)) or blocked Ca 2+ channels (e.g. (Va)). Compound (Vd) shows a dual mechanism by blocking both channels. -

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