Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor

E W van Tilburg; P A van der Klein; M de Groote; M W Beukers; A P IJzerman

doi:10.1016/s0960-894x(01)00356-0

Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor

Bioorg Med Chem Lett. 2001 Aug 6;11(15):2017-9. doi: 10.1016/s0960-894x(01)00356-0.

Authors

E W van Tilburg¹, P A van der Klein, M de Groote, M W Beukers, A P IJzerman

Affiliation

¹ Leiden/Amsterdam Center for Drug Research, Division of Medicinal Chemistry, PO Box 9502, 2300 RA, Leiden, The Netherlands.

PMID: 11454470
DOI: 10.1016/s0960-894x(01)00356-0

Abstract

The synthesis and receptor binding of novel adenosine receptor antagonists is described. We found that non-xanthine 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives may have high affinity and substantial selectivity for the adenosine A(1) receptor.

MeSH terms

Animals
Cells, Cultured
Humans
Protein Binding / physiology
Purinergic P1 Receptor Antagonists*
Rats
Receptor, Adenosine A2A
Receptor, Adenosine A3
Receptors, Purinergic P1 / drug effects*
Thiazoles / chemical synthesis
Thiazoles / pharmacology*
Visual Cortex / cytology
Visual Cortex / metabolism

Substances

Purinergic P1 Receptor Antagonists
Receptor, Adenosine A2A
Receptor, Adenosine A3
Receptors, Purinergic P1
Thiazoles