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J Med Chem. 2008 Sep 25;51(18):5875-9. doi: 10.1021/jm800586p. Epub 2008 Aug 26.

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.

Author information

1
Dipartimento di Scienze Farmaceutiche, UniVersità di Ferrara, Ferrara, Italy. rmr@unife.it, baraldi@unife.it

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.

PMID:
18729349
DOI:
10.1021/jm800586p
[Indexed for MEDLINE]

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