Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor

Journal of Medicinal Chemistry
Romeo RomagnoliPier Andrea Borea

Abstract

The synthesis and evaluation of a series of 2-amino-3-(4-chlorobenzoyl)-4-[4-(alkyl/aryl)piperazin-yl]thiophene derivatives as allosteric enhancers of the A 1-adenosine receptor are described. The nature of substituents on the phenyl ring tethered to the piperazine seem to exert a fundamental influence on the allosteric enhancer activity, with the 4-chlorophenyl 8f and 4-trifluoromethyl 8j derivatives being the most active compounds in binding (saturation and displacement experiments) and functional cAMP studies.

References

Jan 11, 2002·Journal of Medicinal Chemistry·C Elisabet TranbergRay A Olsson
Feb 21, 2003·Journal of Medicinal Chemistry·Pier Giovanni BaraldiPier Andrea Borea
May 2, 2003·Journal of Medicinal Chemistry·Henning LütjensPeter J Scammells
Jun 25, 2005·Mini Reviews in Medicinal Chemistry·Zhan-Guo GaoKenneth A Jacobson
Mar 22, 2007·Cellular and Molecular Life Sciences : CMLS·G Burnstock
Mar 31, 2007·Cell Death and Differentiation·B B Fredholm
Jun 23, 2007·Mini Reviews in Medicinal Chemistry·Pier Giovanni BaraldiRomeo Romagnoli

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Citations

Dec 5, 2009·Journal of Combinatorial Chemistry·Kan WangAlexander Dömling
Jul 7, 2015·Future Medicinal Chemistry·Romeo RomagnoliKatia Varani
Jun 18, 2017·Journal of the American Chemical Society·Andrea NittiDario Pasini
Jul 24, 2010·Expert Opinion on Therapeutic Patents·Neil J Press, John R Fozard
Dec 23, 2008·Organic Letters·Fabian M Piller, Paul Knochel
Aug 15, 2018·Journal of Medicinal Chemistry·Eric A WoldJia Zhou
Jul 6, 2010·Biochimica Et Biophysica Acta·Anikó Göblyös, Ad P Ijzerman

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