2. Academic Validation
  3. New irreversible adenosine A(1) antagonists based on FSCPX

New irreversible adenosine A(1) antagonists based on FSCPX

  • Bioorg Med Chem Lett. 2002 Nov 4;12(21):3179-82. doi: 10.1016/s0960-894x(02)00639-x.
Anthony R Beauglehole 1,  Stephen P Baker,  Peter J Scammells
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Victorian College of Pharmacy, Monash University, 381 Royal Parade, Parkville, Victoria 3052, Australia.
PMID: 12372528 DOI: 10.1016/s0960-894x(02)00639-x
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.

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