title: Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays.
abstract: Evaluation of a biased "library" of pyrrolo[2,3-d]pyrimidines using yeast-based functional assays expressing human A1- and A2a-adenosine receptors, led to the A1 selective antagonist 4b. A direct correlation between yeast functional activity and binding data was established. Practical compounds with polar residues at C-4 of the pyrrolopyrimidine system required H-bond donor functionality for high potency.
authors.affiliation: Cadus Pharmaceutical Corporation, Tarrytown, NY 10591, USA.
authors.forename: R M
authors.initials: RM
authors.lastname: Campbell
authors.forename: C
authors.initials: C
authors.lastname: Cartwright
authors.forename: W
authors.initials: W
authors.lastname: Chen
authors.forename: Y
authors.initials: Y
authors.lastname: Chen
authors.forename: E
authors.initials: E
authors.lastname: Duzic
authors.forename: J M
authors.initials: JM
authors.lastname: Fu
authors.forename: M
authors.initials: M
authors.lastname: Loveland
authors.forename: R
authors.initials: R
authors.lastname: Manning
authors.forename: B
authors.initials: B
authors.lastname: McKibben
authors.forename: C M
authors.initials: CM
authors.lastname: Pleiman
authors.forename: L
authors.initials: L
authors.lastname: Silverman
authors.forename: J
authors.initials: J
authors.lastname: Trueheart
authors.forename: D R
authors.initials: DR
authors.lastname: Webb
authors.forename: V
authors.initials: V
authors.lastname: Wilkinson
authors.forename: D J
authors.initials: DJ
authors.lastname: Witter
authors.forename: X
authors.initials: X
authors.lastname: Xie
authors.forename: A L
authors.initials: AL
authors.lastname: Castelhano
mesh_terms: D001667:Binding, Competitive; D002460:Cell Line; D006801:Humans; D006860:Hydrogen Bonding; D058915:Purinergic P1 Receptor Antagonists; D011743:Pyrimidines / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D011869:Radioligand Assay; D018047:Receptors, Purinergic P1 / Q000235:genetics / Q000378:metabolism; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism; D012441:Saccharomyces cerevisiae / Q000235:genetics*
chemical_list: D058915:Purinergic P1 Receptor Antagonists; D011743:Pyrimidines; D018047:Receptors, Purinergic P1; D011994:Recombinant Proteins