Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor.
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.
van Tilburg
E W
EW
Leiden/Amsterdam Center for Drug Research, Division of Medicinal Chemistry, PO Box 9502, 2300 RA, Leiden, The Netherlands.
van der Klein
P A
PA
de Groote
M
M
Beukers
M W
MW
IJzerman
A P
AP
D000818:Animals; D002478:Cells, Cultured; D006801:Humans; D011485:Protein Binding / Q000502:physiology; D058915:Purinergic P1 Receptor Antagonists; D051381:Rats; D043705:Receptor, Adenosine A2A; D043684:Receptor, Adenosine A3; D018047:Receptors, Purinergic P1 / Q000187:drug effects*; D013844:Thiazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D014793:Visual Cortex / Q000166:cytology / Q000378:metabolism
D058915:Purinergic P1 Receptor Antagonists; D043705:Receptor, Adenosine A2A; D043684:Receptor, Adenosine A3; D018047:Receptors, Purinergic P1; D013844:Thiazoles