Antagonists of the human A(2A) receptor. Part 5: Highly bio-available pyrimidine-4-carboxamides.
A novel series of antagonists of the human A(2A) receptor have been identified and have been shown to display good potency and high degrees of selectivity over other receptor sub-types. Displaying in vivo potency in commonly used disease models and high oral bio-availability, this class of compounds may serve as clinically useful treatments for the relief of the symptoms associated with Parkinson's disease.
Gillespie
Roger J
RJ
Vernalis (R+D) Ltd., Winnersh Wokingham, UK.
Bamford
Samantha J
SJ
Gaur
Suneel
S
Jordan
Allan M
AM
Lerpiniere
Joanne
J
Mansell
Howard L
HL
Stratton
Gemma C
GC
D058917:Adenosine A2 Receptor Antagonists; D000284:Administration, Oral; D000577:Amides / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry; D000818:Animals; D004195:Disease Models, Animal; D006801:Humans; D051379:Mice; D011743:Pyrimidines / Q000737:chemistry*; D043705:Receptor, Adenosine A2A / Q000378:metabolism
D058917:Adenosine A2 Receptor Antagonists; D000577:Amides; D011743:Pyrimidines; D043705:Receptor, Adenosine A2A