Published in

Elsevier, Bioorganic and Medicinal Chemistry Letters, 21(12), p. 3179-3182, 2002

DOI: 10.1016/s0960-894x(02)00639-x

Wiley-VCH Verlag, ChemInform, 9(34), 2003

DOI: 10.1002/chin.200309153

Links

Tools

Export citation

Search in Google Scholar

New irreversible adenosine A1 antagonists based on FSCPX

Journal article published in 2002 by Anthony R. Beauglehole, Stephen P. Baker, Peter John Scammells ORCID
This paper was not found in any repository, but could be made available legally by the author.
This paper was not found in any repository, but could be made available legally by the author.

Full text: Unavailable

Green circle
Preprint: archiving allowed
Upload
Orange circle
Postprint: archiving restricted
Upload
Red circle
Published version: archiving forbidden
Policy details
Data provided by SHERPA/RoMEO

Abstract

FSCPX (1) and its amide analogue (2) have been reported to exhibit potent and selective irreversible antagonism of the A(1) adenosine receptor (A(1)AR) when used in in vitro biological preparations. In order to obtain an irreversible A(1)AR antagonist with improved stability, analogues of FSCPX incorporating the chemoreactive 4-(fluorosulfonyl)phenyl moiety separated from the xanthine pharmacophore by a ketone linkage were explored. Compounds 4a-c exhibited improved affinity for the A(1)AR and concentration-dependent irreversible binding to the A(1)AR.