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Synthesis and biological evaluation of thiophene derivatives as acetylcholinesterase inhibitors.

ABSTRACT: A series of new thiophene derivatives has been synthesized using the Gewald protocol. The acetylcholinesterase inhibition activity was assayed according to Ellman's method using donepezil as reference. Some of the compounds were found to be more potent inhibitors than the reference. 2-(2-(4-(4-Methoxyphenyl)piperazin-1-yl)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide (IIId) showed 60% inhibition, compared to only 40% inhibition by donepezil.

SUBMITTER: Ismail MM

PROVIDER: S-EPMC6268334 | biostudies-literature | 2012 Jun

REPOSITORIES: biostudies-literature

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Synthesis and biological evaluation of thiophene derivatives as acetylcholinesterase inhibitors.

Ismail Mohamed M MM Kamel Mona M MM Mohamed Lamia W LW Faggal Samar I SI Galal Mai A MA

Molecules (Basel, Switzerland) 20120612 6

A series of new thiophene derivatives has been synthesized using the Gewald protocol. The acetylcholinesterase inhibition activity was assayed according to Ellman's method using donepezil as reference. Some of the compounds were found to be more potent inhibitors than the reference. 2-(2-(4-(4-Methoxyphenyl)piperazin-1-yl)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide (IIId) showed 60% inhibition, compared to only 40% inhibition by donepezil. ...[more]

PMID: 22692245

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