2-Aminothiazoles: a new class of agonist allosteric enhancers of A(1) adenosine receptors.
This report describes the synthesis and structure-activity relationships of a new class of A(1) adenosine receptor agonist allosteric enhancers, 2-aminothiazolium salts. The EC(50) of compounds 6a, 6b, 7, and 8 were 0.3, 4.5, 3.8, and 1.2 microM, substantially lower than that of the 'Gold Standard' 2-amino-3-benzoyl thiophene (PD 81,723), which has an EC(50) of 38 microM.
Chordia
Mahendra D
MD
Department of Chemistry, University of Virginia, Charlottesville, VA 22901, USA. mdc3x@virginia.edu
Murphree
Lauren J
LJ
Macdonald
Timothy L
TL
Linden
Joel
J
Olsson
Ray A
RA
D000494:Allosteric Regulation; D006801:Humans; D058906:Purinergic P1 Receptor Agonists; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
D058906:Purinergic P1 Receptor Agonists; D013844:Thiazoles; C004483:2-aminothiazole