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Bioorg Med Chem Lett. 2001 May 21;11(10):1333-7.

Ring-Constrained (N)-methanocarba nucleosides as adenosine receptor agonists: independent 5'-uronamide and 2'-deoxy modifications.

Author information

1
Molecular Recognition Section, LBC, NIDDK, National Institutes of Health, Bethesda, MD 20892, USA.

Abstract

Novel methanocarba adenosine analogues, having the pseudo-ribose northern (N) conformation preferred at adenosine receptors (ARs), were synthesized and tested in binding assays. The 5'-uronamide modification preserved [N6-(3-iodobenzyl)] or enhanced (N6-methyl) affinity at A3ARs, while the 2'-deoxy modification reduced affinity and efficacy in a functional assay.

PMID:
11392549
PMCID:
PMC4957017
DOI:
10.1016/s0960-894x(01)00213-x
[Indexed for MEDLINE]
Free PMC Article

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